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抑制剂选择性比较

特异性亚型抑制剂

PI3K产品

所有产品 PI3K抑制剂(77) PI3K激活剂(1) 新PI3K产品

产品目录	产品描述	文献引用	实验数据
S1009	Dactolisib (BEZ235, NVP-BEZ235) Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。在 3T3^TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。	Cancer Cell, 2019, 35(5):752-766 Cancer Res, 2019, 79(1):209-219 Cell Rep, 2019, 27(3):820-834	Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.
S1065	Pictilisib (GDC-0941) Pictilisib (GDC-0941) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Phase 2。	Nat Med, 2019, 25(5):838-849 Clin Cancer Res, 2019, 10.1158/1078-0432 Cancer Res, 2019, 79(6):1138-1150	TGF-β induces mTORC2 activation. ( A ) NMuMG cells were treated with TGF-β for the indicated times before lysis and immunoblotting. (B ) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to anti-Rictor immunoprecipitation, and the immunoprecipitates were subjected to in vitro kinase assays using kinase-inactive Akt1 as a substrate, before immunoblotting of the kinase reactions, immunoprecipitates and cell lysates. The left panels are from the same gel, without differential exposure. ( C ) NMuMG cells were treated or not with TGF-β or insulin for the indicated times, in the presence or absence of SB431542 or GDC-0941. The kinase activity of mTORC2 was then assessed as in B. The top panels are from the same gel, without differential exposure. (D) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to immunoprecipitation using Rictor antibody, and/or immunoblotted.
S1105	LY294002 LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。	Cell, 2019, 176(6):1379-1392 Nat Cell Biol, 2019, 21(2):226-237 Clin Cancer Res, 2019, 25(5):1639-1649	Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
S2226	Idelalisib (CAL-101, GS-1101) Idelalisib (CAL-101, GS-1101) 是选择性p110δ抑制剂，在无细胞试验中IC50为 2.5 nM；对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍，对p110δ的选择性是对 C2β，hVPS34，DNA-PK 和 mTOR的400到4000倍。	Leukemia, 2019, 10.1038/s41375-019-0486-9 Am J Transplant, 2019, 19(5):1305-1314 Epigenetics, 2019, 1-16	293T cells were transfected with HA-tagged Fbxo45. At 48 h after transfection, cells were treated with AKT inhibitor (CAL-101; 10 uM, 4 h), cell extracts from the cytoplasm or nuclei were subjected to IP with anti-HA resin followed by western blot analysis with indicated antibodies.
S2247	Buparlisib (BKM120, NVP-BKM120) Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34，mTOR，DNAPK 的作用效果下降，而对 PI4Kβ几乎没有活性。Phase 2。	Science, 2019, 364(6441) Nat Cell Biol, 2019, 21(2):226-237 Nat Commun, 2019, 10(1):2910	AN3CA (A) and JHUEM2 (B) cells were treated for the indicated times with DMSO, 0.3 μM BGJ398 (BGJ), 0.3 μM GDC-0941 (GDC), 0.6 μM BYL719 (BYL) and 0.6 μM BKM120 (BKM) alone or in combination. Cell lysates were immunoblotted with antibodies for phospho-AKT (Ser473), total AKT, phospho-ERK (Thr202/Tyr204), ERK2, phospho-S6 (Ser240/244), total S6, phospho-4EBP1 (Thr37/46), total 4EBP1, total PARP and cleaved PARP. Tubulin was detected as the loading control. Western blot analysis of AN3CA and JHUEM2.
S6541^New	MTX-211 MTX-211是PI3K和EGFR的双重抑制剂。
S6516^New	GNE-477 GNE-477是有效的PI3K/mTOR抑制剂，对PI3Kα的IC50值为4 nM，对mTOR的K_iapp值为21 nM。
S8693^New	Selective PI3Kδ Inhibitor 1 (compound 7n) Selective PI3Kδ Inhibitor 1 (compound 7n)是PI3Kδ抑制剂，对PI3Kδ的IC50为0.9 nM，其选择性比对其他I类PI3K亚型高1000倍以上。Selective PI3Kδ Inhibitor 1对PI3Kα/γ/β的IC50值分别为3670、1460、21300 nM。
S5818^New	acalisib (GS-9820) acalisib (GS-9820)是一种具有高度选择性的、有效的p110δ抑制剂，IC50为14 nM。它对p110δ的选择性是对其他I类PI3K酶的选择性的114-400倍，对II类和III类PI3K酶和其他PI3K相关蛋白（包括mTOR和DNA-PK）没有活性。
S8752^New	leniolisib(CDZ 173) Leniolisib(CDZ 173)是有效的选择性PI3Kδ抑制剂，对PI3Kα, PI3Kβ, PI3Kγ和PI3Kδ的IC50分别为0.244, 0.424, 2.23和0.011 μM。
S8738^New	Bimiralisib (PQR309) Bimiralisib (PQR309)是一种新型的、可渗透入大脑的PI3K/mTOR双重抑制剂，在体内外具有抗淋巴瘤活性。相对于其他PI3K相关性脂质激酶、蛋白激酶和非相关性靶点，它对PI3K/mTOR具有较高选择性。
S8560^New	Seletalisib (UCB-5857) Seletalisib是新型的PI3Kδ小分子抑制剂，IC50为12 nM。它对PI3K具有显著的选择性，相对其他I型PI3K亚型，Seletalisib对PI3Kδ的选择性高24-303倍。
S1038	PI-103 PI-103是一种多靶点 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50为 2 nM/3 nM/3 nM/15 nM，对 mTOR/DNA-PK的作用较小，IC50为30 nM/23 nM。	Mol Cancer Ther, 2018, 17(6):1259-1270 Int J Oncol, 2018, 52(6):2051-2060 Int J Oncol, 2018, 52(3):828-840	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
S2638	NU7441 (KU-57788) NU7441 (KU-57788)是一种高度有效的，选择性DNA-PK抑制剂，在无细胞试验中IC50为14 nM，也会抑制PI3K，IC50为5 μM。它可降低NHEJ的频率，而增强Cas9介导DNA剪接后发生的同源重组修复率。	FASEB J, 2019, 33(6):6778-6788 Mol Biol Rep, 2019, 10.1007/s11033-019-04605-0 FEBS Open Bio, 2019, 9(7):1315-1326	Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
S1169	TGX-221 TGX-221 是一种p110β-特定的抑制剂，在无细胞试验中IC50为 5 nM，作用于p110β的选择性是作用于p110α的1000倍。	Cell Metab, 2019, 29(6):1400-1409 Mol Cell Proteomics, 2019, 18(4):669-685 Mol Cancer Ther, 2018, 17(10):2091-2099	A p110β-selective antagonist rescues increased protein synthesis in synaptic fractions from Fmr1 KO mice and in LCLs from a patient with FXS. (A–C) Treatment of synaptoneurosomes with TGX-221 (1 μmol/L, 30 min) reduces p110β-specific PI3K activity and phosphorylation of the downstream target AKT in both WT and Fmr1 KO SNS, shown by a radioactive PI3K assay and phosphoAkt- specific western blot-ting (A). (B) Quantification of PI3K activity using a competitive ELISA showed a significant reduction in PI3K activity in both genotypes after treatment [ n = 4, 2-way ANOVA, P (genotype) = 0.0086, P (treatment) = 0.0087, P (interaction) = 0.7154]. (C) Densitometric quantification of phosphoAkt-specific western blots showed a significant effect of treatment (C, n = 4, 2-way ANOVA, *P (treatment) = 0.0005, P (genotype) =0.372, P (interaction) = 0.4894).
S1268	IC-87114 IC-87114是一种选择性的PI3Kδ抑制剂，无细胞试验中IC50为0.5 μM，作用于PI3Kδ比作用于PI3Kγ和PI3Kα/β选择性分别高58和100倍。	Int J Oncol, 2018, 52(3):828-840 Am J Transplant, 2016, 16(9):2624-38 Cancer Cell, 2015, 27(1):97-108
S2758	Wortmannin Wortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。也会抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。	Cell, 2019, 176(6):1379-1392 Nat Cell Biol, 2019, 21(2):226-237 Theranostics, 2019, 9(15):4375-4390	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
S1118	XL147 analogue XL147 analogue是一种选择性的，可逆的I型PI3K抑制剂，作用于PI3Kα/δ/γ，无细胞试验中IC50分别为39 nM/36 nM/23 nM，对PI3Kβ作用效果稍弱。Phase 1/2。	Oncogene, 2015, 10.1038/onc.2015.143 Cancer Res, 2014, 74(18):5184-94 PLoS One, 2014, 9(8):e105280	Breast cancer cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of XL147 for 24 hours.
S1072	ZSTK474 ZSTK474抑制I型PI3K亚型，在无细胞试验中IC50为37 nM，对PI3Kδ作用最显著。Phase 1/2。	Leukemia, 2018, 32(1):159-167 J Cell Physiol, 2018, 233(3):1796-1811 NAT MATER, 2017, 10.1038/NMAT5024	Representative Western blot of Erk1/2, phospho-Erk1/2, Akt, phospho-Akt antibodies in BCPAP, K1 and 8505C cells treated at 4 h using IC50 doses. 1, cells untreated; 2, cells treated with RAF265; 3, cells treated with ZSTK474; 4, cells treated with SB590885; 5, cells treated with RAF265+ZSTK474; 6, cells treated with SB590885+ZSTK474.
S2814	Alpelisib (BYL719) Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。	Science, 2019, 364(6441) Nat Med, 2019, 25(5):838-849 Cell Rep, 2019, 27(1):294-306	BYL719 induces Apoptosis in MM cells. The effect of increasing concentrations of BYL719 (0-2.5 umol/l) for 48 h on the apoptosis of MM1s cells. The effect of BYL719 on the apoptosis signalling; cleaved PARP, caspase 3, caspase 9 by Western blotting. MM, multple myeloma.
S1410	AS-605240 AS-605240选择性抑制PI3Kγ，IC50为8 nM，作用于PI3Kγ比作用于PI3Kδ/β和PI3Kα选择性分别高30和7.5倍以上。	Cell Rep, 2019, 27(2):631-647 Oncol Lett, 2018, 15(2):2105-2110 Cell Host Microbe, 2017, 21(5):611-618	After starved in serum-free medium for 24 h, Breast cancer cells incubated with the indicated concentrations of AS-605240 for 3 h,followed by 15-minute stimolation of 100ng/ml EGF
S1205	PIK-75 HCl PIK-75 HCl是一种p110α抑制剂，IC50为5.8 nM (比作用于p110β效果强200倍)，在Ser773处功能特异性突变，也有效抑制DNA-PK，无细胞试验中IC50为2 nM。	Cancer Cell, 2019, 35(5):752-766 Cell Metab, 2019, 29(6):1400-1409 Mol Cell Proteomics, 2019, 18(4):669-685	A549 cells were treated with DMSO or PIK-75 (200 nM) for 1 h and subsequently stimulated with izTRAIL for 24 h. Long-term survival was visualized after 7 days by crystal violet staining. One of two independent experiments is shown.
S2767	3-Methyladenine (3-MA) 3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。现配现用（加热助溶）。	Acta Neuropathol, 2019, 138(1):67-84 Cell Rep, 2019, 27(7):2075-2091.e5 Cell Death Differ, 2019, 26(6):1077-1088	granulosa cells (GCs) with 24 h of melatonin (10 μM) treatment were rinsed in PBS, and then exposed to H2O2 (200 μM) for 2 h. The autophagy inhibitor 3-MA (10 mM), or the apoptosis inhibitor Z-VAD-FMK (50 μM) were added 1 h prior to H2O2 incubation. Cell viability was determined using the CCK-8 assay. Data represent mean ± S.E; n = 3 in each group. P < 0.05 (*P < 0.01) vs. vehicle group at 0 h. # Represents P < 0.05 (## Represents P < 0.01) vs. H2O2-only-treated cells. & Represents P > 0.05 vs. H2O2-only-treated cells. N, not significant, P > 0.05. δ Represents P < 0.05 (δδ Represents P < 0.01) vs. Z-VAD-FMK-treated cells.
S2636	A66 A66是一种有效的特异性p110α抑制剂，无细胞试验中IC50为32 nM，作用于p110α比作用于其他I类PI3K亚型选择性高100多倍。	Int J Cancer, 2019, 145(3):817-829 Mol Cell Biochem, 2018, 439(1-2):199-211 Cancer Immunol Res, 2017, 5(8):695-709	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of A66 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S1523	Voxtalisib (SAR245409, XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue是作用于mTOR/PI3K的双重抑制剂，对p110γ作用最强，IC50为9 nM；也可抑制DNA-PK和mTOR。Phase 1/2。	Cell Rep, 2015, 11(3):446-59 Mol Cancer Res, 2014, 12(5):703-13 Am J Transl Res, 2014, 6(5):471-493	The TMZ/XL765 combination decreases serum GH and PRL of mice bearing GH3 xenografts. A and B, After treatment with DMSO, TMZ, XL765, or the XL765/TMZ combination, the blood of the nude mice xenograft with GH3 tumor was collected and serum rat-GH and rat-PRL were measured by IRMA (TMZ/XL765 combination vs TMZ or XL765 alone: ***P <.001).
S2658	Omipalisib (GSK2126458, GSK458) Omipalisib (GSK2126458, GSK458)是一种高选择性的，有效的p110α/β/γ/δ和 mTORC1/2抑制剂，无细胞试验中K_i分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。Phase 1。	Clin Cancer Res, 2019, 25(5):1639-1649 Cancer Genomics Proteomics, 2018, 15(4):239-248 Cancer Lett, 2017, 406:47-53
S1187	PIK-90 PIK-90是一种PI3Kα/γ/δ抑制剂，IC50分别为11 nM/18 nM/58 nM，对PI3Kβ作用效果稍弱。	Int J Oncol, 2018, 52(3):828-840 Exp Mol Med, 2015, 47:e143 Biochim Biophys Acta, 2015, 1853(10 Pt A):2570-9	Tyr(P)^Irs1 determined in CHO^IR/Irs1 cells treated with kinase inhibitors. Cells were treated for 30 min without or with PIK-90 at concentrations increasing sequentially 2-fold between the boundaries shown in Fig. 4 before incubation with insulin (30 nM, 30 min). Cleared lysates were subject to immunoblotting with antibodies against Irs1 or Tyr(P). The bands were quantified on a Kodak Image Station 4000MM Pro, and the data were analyzed using Carestream Molecular Imaging software version 5.0.
S1462	AZD6482 AZD6482是一种PI3Kβ抑制剂，无细胞试验中IC50为10 nM，作用于PI3Kβ比作用于PI3Kδ， PI3Kα和PI3Kγ选择性分别高8，87和109倍。Phase 1。	Mol Cancer Res, 2017, 10.1158/1541-7786.MCR-16-0183 Breast Cancer Res, 2016, 10.1186/s13058-016-0697-1 Thromb Haemost, 2016, 115(6):1138-46	Cells treated with either control or INPP4B siRNA and following a 1-hour treatment with either DMSO or 1 mmol/L inhibitor; pPRAS40T246 and total PRAS40 were run on a separate blot for which the bottom Ku-86 panel is the loading control(pan-PI3Ki: GDC-0941, PI3K-ai: BYL719,PI3K-bi: AZD6482)
S2743	PF-04691502 PF-04691502是一种ATP竞争性的PI3K(α/β/δ/γ)/mTOR双重抑制剂，在无细胞试验中K_i为1.8 nM/2.1 nM/1.6 nM/1.9 nM和16 nM，对Vps34， AKT， PDK1， p70S6K， MEK， ERK， p38 和 JNK 几乎没有作用活性。Phase 2。	Onco Targets , 2018, 11:943-953 Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-16-1971 Int J Oncol, 2016, 48(1):253-60	BMDMs from WT animals were treated with different concentrations of PI3K inhibitors (500 nmol/L PF4691502, PI-103, BKM120 and 25 μmol/L SF1126) followed by hypoxia for 4 hours for Western blots. These macrophages were either used for lysate preparation (nuclear extracts for HIFα or WCE for pAKT and AKT) and Western blot analysis.
S2696	Apitolisib (GDC-0980, RG7422) Apitolisib (GDC-0980, RG7422)是一种有效的，I型PI3K抑制剂，作用于PI3Kα/β/δ/γ，无细胞试验中IC50分别为5 nM/27 nM/7 nM/14 nM，也是mTOR抑制剂，无细胞试验中K_i为17 nM，比作用于其他PIKK家族激酶选择性高。Phase 2。	Cell Death Dis, 2019, 10(3):231 Leukemia, 2018, 10.1038/s41375-018-0012-5 Oncogene, 2016, 35(38):5070-7	Immunoblots from AR + TNBC cell lines treated with either CDX (25 uM), GDC-0941 (300 nM) or GDC0980 (100 nM) as single agents or CDX in combination with either GDC-0941 or GDC-0980 for 48 h analyzed for AR, p-AKT, AKT, p-S6, S6 and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) protein.
S1360	GSK1059615 GSK1059615是一种PI3Kα/β/δ/γ (可逆的)和mTOR的双重抑制剂，IC50分别为0.4 nM/0.6 nM/2 nM/5 nM和12 nM。Phase 1。	Cell Rep, 2019, 27(3):820-834 Int J Oncol, 2018, 52(3):828-840 BMC Cancer, 2017, 17(1):199	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of GSK1059615 for 24 hours.
S7028	Duvelisib (IPI-145, INK1197) Duvelisib (IPI-145, INK1197) 是一种新型选择性PI3K δ/γ抑制剂，在无细胞试验中K_i和IC50分别为 23 pM/243 pM 和 1 nM/50 nM，对 PI3K δ/γ 的选择性比对其它蛋白激酶高。Phase 3。	Leukemia, 2019, 10.1038/s41375-019-0486-9 Cell Rep, 2019, 27(2):631-647 Lab Invest, 2019, 99(5):648-658	PI3K inhibitor IPI-145 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range.
S2628	Gedatolisib (PF-05212384, PKI-587) Gedatolisib (PF-05212384, PKI-587)是一种高度有效的，双重PI3Kα，PI3Kγ和mTOR抑制剂，无细胞试验中IC50分别为0.4 nM， 5.4 nM和1.6 nM。Phase 2。	Mol Cancer Ther, 2016, 15(3):412-20 Clin Cancer Res, 2015, 21(12):2792-801 Cell Rep, 2015, 11(3):446-59	PI3K inhibitors promote apoptosis in checkpoint-defective cell lines. Two checkpoint-functional (A2058, D28) and three defective (HT144, D20, SKMel13) melanoma cell lines growth as tumour spheres as in Figure 4B were either untreated or treated with 5 uM PF-05212384 for 72 h, harvested and immunoblotted for pAkt Ser473.
S1352	TG100-115 TG100-115是一种PI3Kγ/δ抑制剂，IC50为83 nM/235 nM，对PI3Kα/β几乎没有抑制效果。Phase 1/2。	Int J Oncol, 2018, 52(3):828-840 Biochim Biophys Acta, 2017, 1861(4):947-957 Biochim Biophys Acta, 2017, 1861(4):947-957	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
S2671	AS-252424 AS-252424是一种新型，有效的PI3Kγ抑制剂，无细胞试验中IC50为30 nM，作用于PI3Kγ比作用于PI3Kα选择性高30倍，对PI3Kδ/β具有低的抑制活性。	Inflammation, 2017, 40(2):435-441 Immunol Res, 2015, 10.1007/s12026-015-8648-y Blood, 2014, 123(2):239-51	Effects of AS252424 on KL-induced cPLA 2 phosphorylation in BMMCs. BMMCs were pre-incubated with AS252424 for 1 h followed by stimulation with KL for 15 min. The phosphorylation of cPLA 2 was evaluated via immunoblot analysis. Results are representative of three independent experiments.P<0.05, P<0.01, **P<0.001 and ### P<0.001, compared with BMMCs with KL induction but without pretreatment by AS252424.
S2749	BGT226 maleate (NVP-BGT226 maleate) BGT226 (NVP-BGT226)是一种新型I型PI3K/mTOR抑制剂，作用于PI3Kα/β/γ，IC50为4 nM/63 nM/38 nM。Phase 1/2。	Oncotarget, 2016, 7(48):79842-79853 Mol Cancer Ther, 2015, 14(8):1928-38 Oncotarget, 2015, 6(19):17147-60	IGROV1-R10 cells were treated with BGT266(250nM) for 8 h.The effect of BGT226 on PI3K/Akt/mTOR pathway activation (A) and on expression of Mcl-1 and Bim (B).
S2759	CUDC-907 CUDC-907是一种PI3K和HDAC双重抑制剂，作用于PI3Kα和HDAC1/2/3/10，IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。Phase 1。	EBioMedicine, 2018, 28:80-89 J Cell Mol Med, 2018, 10.1111/jcmm.13935 Biochem Pharmacol, 2018, 148:13-26	Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 for uninduced cells (a), adipocyteinduced hMSCs exposed to the vehicle control (b) or CUDC-907-treated cells (500 nM) (c). Nile red staining (d and e) on day 7 of post-adipocytic induction in hMSCs and after exposure to CUDC-907. Images were captured at ×20 magnification using the FLoid Cell Imaging Station. The level of Nile red staining was quantified using the Molecular Devices M5 Microplate Reader (f). Data are presented as mean ± S.E (n = 16) from three independent experiments, ***P <0.0005.
S2227	PIK-294 PIK-294是一种高度选择性p110δ抑制剂，IC50为10 nM，作用于PI3Kα/β/γ效果分别低1000，49和16倍。	Cell Metab, 2019, 29(6):1400-1409 Mol Cell Biol, 2012, 32(12):2268-78	After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PIK-294 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
S2681	AS-604850 AS-604850是一种选择性的，ATP竞争性的PI3Kγ抑制剂，IC50为250 nM，作用于PI3Kγ比作用于PI3Kδ/β选择性高80倍以上，作用于PI3Kγ比作用于PI3Kα选择性高18倍。	Nature, 2017, 542(7642):489-493 J Biol Chem, 2014, 289(46):32109-20	Representative blots of activated Rac1 and total Rac1 in response to high glucose shown in cells treated overnight with either DMSO or AS604850 (1 umol/liter).
S8002	GSK2636771 GSK2636771是一种口服生物有效的PI3Kβ选择性抑制剂，其对PI3Kβ的选择性比对PI3Kα/PI3Kγ高900倍以上，比对PI3Kδ的选择性大10倍以上。对PTEN缺失细胞系敏感。	Cell Signal, 2019, 53:122-131 Cancer, 2018, 124(18):3693-3705 FASEB J, 2018, 10.1096/fj.201800183R	Cells were treated as indicated. Medium and drug were refreshed every 2 to 3 days, and protein lysates were analyzed as above.
S2802	Copanlisib (BAY 80-6946) Copanlisib (BAY 80-6946)是一个高效的泛I型 PI3K抑制剂，其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3。	Cell Death Discov, 2019, 5:86 Nature, 2018, 560(7719):499-503 Biomed Res Int, 2018, 2018:1023490	The compounds BAY80-6946 and TG100713, which are respectively an alpha/beta- and a pan-isoforms inhibitors, demonstrated a very good ability to block Jurkat E6.1 proliferation with an IC50 slightly higher than 1 mM.
S2699	CH5132799 CH5132799抑制I型PI3Ks，尤其是PI3Kα，IC50为14 nM；对PI3Kβδγ作用效果稍弱，对PIK3CA突变型细胞系敏感。Phase 1。	Biochimie, 2014, 105:182-91 Am J Transl Res, 2014, 6(5):471-493	Effect of selected compounds on MLC phosphorylation induced by 2-AG. Washed platelets (1.0 x 10⁹ platelets/mL) were preincubated at 37 ℃ for 10 min with saline or 20 uM LY294002 (L), 10 uM CH5132799 (C), 10 uM TGX221 (T), 10 uM MK2206 (M), 20 uM Y27632 (Y), 1 uM PIK-75 (P), 1 U/mL apyrase (AP), 5 uM AS252424 (AS), 1 uM IC87114 (IC) and then stimulated for 30 s with 10 uM 2-AG. At the end of incubation suitable aliquots were immunoblotted with anti-p-MLC (thr18/ser19) as detailed in Methods. Blot is representative of four independent experiments.
S2682	CAY10505 CAY10505是AS-252424的羟基化合物，是一种PI3Kγ抑制剂，IC50为30 nM.	Br J Haematol, 2014, 166(4):529-39	(D) Box plots showing the results of primary MM cell treatment (n = 22; in co-culture with BMSCs) with PI3K inhibitors (10 umol/l each). BYL-719 exerted the strongest anti-myeloma effects of TGX-221, CAY10505 or CAL-101. The mean survival value is indicated by a horizontal bar and the end of the whiskers show the values of the most sensitive and most resistant sample, respectively. (E) Treatment of PBMCs (n = 5) for 5 d with PI3K isoform-specific inhibitors (10 umol/l each).
S2207	PIK-293 PIK-293是一种PI3K抑制剂，最有效作用于PI3Kδ，IC50为0.24 μM，作用于PI3Kα/β/γ效果分别低500，100和50倍。		After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PIK-293 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
S2739	PKI-402 PKI-402是一种有效的，pan-PI3K/mTOR双重抑制剂，靶向作用于PI3Kα/β/γ/δ和mTOR，IC50分别为2 nM/7 nM/16 nM/14 nM和3 nM，也有效作用于PI3Kα突变型E545K和H1047R。	Cancer Lett, 2019, 443:135-144
S2870	TG100713 TG100713是一种pan-PI3K抑制剂，作用于PI3Kγ， PI3Kδ， PI3Kα和PI3Kβ，IC50分别为50 nM， 24 nM， 165 nM和215 nM。	MedChemComm, 2013, 10.1039/c3md00301a	The compounds BAY80-6946 and TG100713, which are respectively an alpha/beta- and a pan-isoforms inhibitors, demonstrated a very good ability to block Jurkat E6.1 proliferation with an IC50 slightly higher than 1 mM.
S7016	VS-5584 (SB2343) VS-5584 (SB2343)是一种有效的，选择性，PI3K/mTOR双重抑制剂，抑制mTOR和PI3Kα/β/δ/γ，IC50分别为3.4 nM和2.6-21 nM。Phase 1。	Biomed Pharmacother, 2018, 428-437 Platelets, 2018, 29(3):277-287 Cell Physiol Biochem, 2018, 47(2):680-693	Effect of VS-5584 on platelet adhesion. A-F: WP (A, B) and PRP (D, E) were treated with DMSO as vehicle (A, D; n = 3) or with 20 nM (B; n = 3) and 20 μM (E; n = 3) of VS-5584 and seeded on siliconized coverslips for the quantitative analysis of WP (C) and PRP adhesion (F). Scale bars: A, B, D, E = 50 μm; Data are given in % of vehicle. Mean ± SEM. p < 0.05 vs. vehicle. G, H: Representative images of WP treated with vehicle (G) or 20 nM of VS-5584 (H). The number of non-spread cells (arrows) is higher in VS-5584-treated WP. Scale bars: 20 μm. I: Quantification of spread platelets based on their morphology. Data are given in % of vehicle. Mean ± SEM. p < 0.05 vs. vehicle.
S7103	Taselisib (GDC 0032) Taselisib (GDC 0032)是一种有效，下一代的β亚型PI3K抑制剂，作用于PI3Kα/δ/γ， IC50分别为0.29 nM/0.12 nM/0.97nM，比作用于PI3Kβ选择性高10倍以上。	Science, 2019, 364(6441) Cell Rep, 2019, 27(1):294-306 Anal Biochem, 2018, 547:66-76
S7018	CZC24832 CZC24832是第一个PI3Kγ选择性抑制剂，IC50为27 nM，比作用于PI3Kβ选择性高10倍，比作用于PI3Kα和PI3Kδ选择性高100倍以上。	Leukemia, 2018, 32(9):1958-1969 Sci Rep, 2018, 8(1):5558 Mol Cancer Ther, 2018, 17(5):1090-1100	(c) MM primary cells were treated with idelalisib (1 μm), CZC24832 (1 μm) and duvelisib (1 μm) for 72 h and then assessed for apoptosis by PI/Annexin V staining (n=4).
S7813	AMG319 AMG319是一种有效的选择性PI3Kδ抑制剂，IC50为18 nM，选择性比作用于其他PI3Ks高47倍多。Phase 2。
S7938	GSK2292767 GSK2292767是一种有效的、选择性的PI3Kδ抑制剂。
S8163	GDC-0084 GDC-0084是一种能透过血脑屏障的PI3K和mTOR的抑制剂，对PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ 和mTOR的Kiapp分别为2 nM, 46 nM, 3 nM, 10 nM和70 nM。
S8157	GDC-0326 GDC-0326是一种有效的、选择性的PI3Kα抑制剂，Ki值为0.2 nM。在酶活性实验中，对PI3Kα的选择性显著高于其它I类亚型。	Microb Cell, 2018, ;5(12):545-554
S7356	HS-173 HS-173 是强效的PI3Kα抑制剂，其IC50为0.8 nM。	Sci Rep, 2018, 8(1):5558 Cancer Cell Int, 2017, 10.1186/s12935-017-0396-8 Cancer Cell Int, 2017, 17:112	b, d Serum-deprived MG-63 (b) and U20S cells (d) were pre-treated with 1 nmol/L HS-173 (PI3Kα inhibitor), 10 nmol/L TGX-221 (PI3Kβ inhibitor), 10 nmol/L CZC24832 (PI3Kγ inhibitor) and 10 nmol/L CAL-101 (PI3Kδ inhibitor) for 1 h, then were incubated with 100 ng/mL Wnt5a and harvested at 30 min after the start of Wnt5a treatment. Data were presented as mean ± SD of 3 determinations. The relative RhoA activity was normalized to the average value of each inhibitor-untreated group
S8589	SF2523 SF2523是一种有效的、具有高度选择性的PI3K抑制剂，对PI3Kα, PI3Kγ, DNA-PK, BRD4 和 mTOR的IC50分别为34 nM, 158 nM, 9 nM, 241 nM 和 280 nM。
S8581	Serabelisib (INK-1117,MLN-1117,TAK-117) Serabelisib (INK-1117,MLN-1117,TAK-117)是一种有效的、选择性的，可用于口服的PI3Kα抑制剂，IC50为21 nM。对PI3Kα的选择性比对其他I类PI3K家族成员高100倍以上。
S8330	IPI-549 IPI-549是PI3K-γ的有效抑制剂，选择性是对其他脂质和蛋白激酶的100倍以上。生化IC50为16 nM。
S2391	Quercetin Quercetin是蔬菜水果和白酒中的天然黄酮类化合物，是一种体外重组Sirt1蛋白的激活剂同时也是PI3K抑制剂，IC50为2.4 – 5.4 μM。	Front Cell Neurosci, 2019, 13:316 Clin Cancer Res, 2018, 10.1158/1078-0432 Mol Nutr Food Res, 2017, 61(4)	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S8456	VPS34 inhibitor 1 (Compound 19, PIK-III analogue) VPS34 inhibitor 1 (Compound 19, PIK-III analogue)是有效的、选择性的VPS34抑制剂，IC50为15 nM。	Oncotarget, 2017, 8(24):38099-38112	Confirmation of selective growth inhibition using VPS34-IN1 inhibitor. Proliferation of Tsc2+/+ and Tsc2-/- MEFs treated with vehicle control (DMSO), CQ (5 uM), VPS34-IN1 (500 nM) or the combination for 72 hours (crystal violet staining). Two sample t-test was carried out between CQ and SAR405 and each drug alone. Results are representative of three independent experiments. Bar graph represent means ±SD.
S7646	Voxtalisib (XL765, SAR245409) Voxtalisib (SAR245409, XL765)是作用于mTOR/PI3K的双重抑制剂，对p110γ作用最强，IC50为9 nM；也可抑制DNA-PK和mTOR。Phase 1/2。	Biomed Pharmacother, 2018, 103:1069-1078 Nat Neurosci, 2017, 20(8):1074-1084 Int J Oncol, 2015, 47(3):1143-59	HL60, HL60/ADR, K562 and K562/A02 cells pretreated with various concentrations of Voxtalisib (0, 0.625, 1.25, 2.5, 5 and 10 μM) for 48 h were harvested for western blot. The levels of cyclin D1, p27, and p-pRb in the nuclei were determined.
S8596	Autophinib Autophinib是有效的自噬 (autophagy)抑制剂，在饥饿诱导的自噬试验和rapamycin诱导的自噬试验中，其IC50分别为90 nM和40 nM。它还是Vps34的抑制剂，IC50为19 nM。	Cell Rep, 2019, 27(12):3413-3421
S7798	GNE-317 GNE-317 是一种有效的，大脑渗透性 PI3K 抑制剂。
S8672	Tenalisib (RP6530) Tenalisib (RP6530)是一种有效的、选择性的PI3Kδ/γ抑制剂，对PI3Kδ和PI3Kγ的IC50值分别为24.5 nM和33.2 nM。它对δ/γ的选择性比对α和β亚型高300倍和100倍以上。
S8194	umbralisib (TGR-1202) TGR-1202是一种新型的PI3Kδ抑制剂，在酶学研究中和在细胞研究中，其抑制PI3Kδ活性的IC50和EC50分别为22.2 nM和24.3 nM。
S7937	Nemiralisib (GSK2269557) Nemiralisib，又名GSK-2269557，是有效的、选择性的PI3Kδ抑制剂（pKi=9.9）。
S8322	LY3023414 LY3023414是一种口服的ATP竞争性抑制剂，抑制I类PI3K亚型、mTOR和DNA-PK。		The structure and formula weight of LY3023414 were presented (A). Established human glioma cells (U251MG and A172 lines), primary human astrocytes (“Astrocytes”) or primary human glioma cells [three lines, “Glioma (L1/2/3)”], were either left untreated (“Ctrl”) or treated with LY3023414 at 1-1000 nM, cells were further cultured for indicated time; Cell survival was tested (B, C, and E) (n=5). Cell proliferation was also tested by the BrdU ELISA assay (D and F) (n=5). *p < 0.05 vs. “Ctrl”. Experiments in this figure were repeated three times.
S7980	VPS34-IN1 Vps34-IN1 是Vps34的抑制剂，在体外实验中所测得的IC50为25 nM, 对1型和2型 PI3K没有显著抑制作用。	Oncotarget, 2017, 8(24):38099-38112	C. Lysosomal and endosomal inhibition selectively targets Tsc2−/− MEFs. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), Vps34 inhibitor (SAR405; 1uM) or the combination for 72 hours (crystal violet staining). D. Confirmation of selective growth inhibition using VPS34-IN1 inhibitor. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), VPS34-IN1 (500nM) or the combination for 72 hours (crystal violet staining). Two-sample t-test was carried out between CQ and SAR405 and each drug alone. Results are representative of three independent experiments. Bar graph represent means ±SD.
S8696	2-D08 2-D08是一种具有细胞透性的蛋白类泛素化（protein sumoylation）抑制剂。它还能抑制Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。
S7335	IPI-3063 IPI-3063是有效的、选择性的p110δ抑制剂，在无细胞实验中，IC50为2.5 ± 1.2 nM。其对其他I型PI3K亚型如p110α, p110β, p110γ的IC50s至少高400倍。
S7682	SAR405 SAR405是一种低分子量的Vps34抑制剂（Kd=1.5 nM），具有高选择性，在浓度高达10 μM时，对I类和Ⅱ类PI3Ks及mTOR没有活性。	Urol Oncol, 2018, 36(4):160.e1-160.e13	RT-112 and RT-112 (CisPt-R) cells were treated with cisplatin, SAR405, and a combination of both in absence and presence of QVD (10 µM). Again, the concentrations used were the IC50 or half IC50 values for RT-112 (CisPt-R) and RT-112, respectively. After 48 hours, the cells were lysed, and cleared cellular lysates were subjected to SDS-PAGE and immunoblotting for PARP, caspase-3 (Casp3), and Actin. One representative immunoblot is shown.
S7683	PIK-III PIK-III, 一种选择性VPS34酶活性的抑制剂，抑制细胞自噬以及LC3的重新脂化，稳定自噬底物。其对VPS34和 PI(3)Kδ的IC50值分别为0.018 μM和1.2 μM。	Cancer Lett, 2018, 435:32-43 Mol Biosyst, 2017, 13(10):1993-2005	LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm
S7623	PI-3065 PI-3065是一种选择性p110δ抑制剂，IC50为15 nM,选择性比其他PI3K家族成员高出70多倍。	Leukemia, 2019, 33(6):1427-1438
S7645	Pilaralisib (XL147) Pilaralisib (XL147)是一种选择性的可逆I型PI3K抑制剂，作用于PI3Kα/δ/γ，在无细胞试验中IC50为 39 nM/36 nM/23 nM，对PI3Kβ作用较低。Phase 1/2。	Cell Rep, 2019, 27(2):631-647 Neoplasia, 2019, 21(6):615-626 J Cell Biochem, 2018, 119(8):6398-6407	I. OMI index decreases in BT474 organoids treated with single and combination therapies at 24 hr. J. OMI index of BT474 organoids treated for 72hr. Red bars denote p<0.05 for treated organoids vs. control. H:trastuzumab (anti-HER2); P:paclitaxel (chemotherapy); XL147 (X).
S7966	AZD8835 AZD8835是一种新型的PI3Kα和PI3Kδ混合型抑制剂，IC50分别为6.2 nM和5.7 nM。对PI3Kβ和PI3Kγ同样具有选择性，IC50分别为431 nM和90 nM。
S8132	Deguelin Deguelin，一种从植物中分离出来的天然产物，是PI3K/Akt的抑制剂。
S7675	PF-4989216 PF-4989216 是一种有效的选择性PI3K抑制剂，对p110α，p110β，p110γ，p110δ，和 VPS34的 IC50 分别为 2 nM，142 nM，65 nM，1 nM，和 110 nM。
S7694	AZD8186 AZD8186是一种有效的选择性PI3Kβ和PI3Kδ抑制剂，IC50分别为 4 nM 和 12 nM。Phase 1。	EBioMedicine, 2018, 28:80-89
S7865	740 Y-P (PDGFR 740Y-P) 740 Y-P是具有细胞可透过性的PI3K磷酸肽激活剂。	J Recept Signal Transduct Res, 2019, 39(1):80-86 Neurochem Res, 2018, 43(6):1210-1226

产品目录	产品描述	文献引用	实验数据
S1009	Dactolisib (BEZ235, NVP-BEZ235) Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。在 3T3^TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。	Cancer Cell,2019, 35(5):752-766 Cancer Res,2019, 79(1):209-219 Cell Rep,2019, 27(3):820-834	Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.
S1065	Pictilisib (GDC-0941) Pictilisib (GDC-0941) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Phase 2。	Nat Med,2019, 25(5):838-849 Clin Cancer Res,2019, 10.1158/1078-0432 Cancer Res,2019, 79(6):1138-1150	TGF-β induces mTORC2 activation. ( A ) NMuMG cells were treated with TGF-β for the indicated times before lysis and immunoblotting. (B ) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to anti-Rictor immunoprecipitation, and the immunoprecipitates were subjected to in vitro kinase assays using kinase-inactive Akt1 as a substrate, before immunoblotting of the kinase reactions, immunoprecipitates and cell lysates. The left panels are from the same gel, without differential exposure. ( C ) NMuMG cells were treated or not with TGF-β or insulin for the indicated times, in the presence or absence of SB431542 or GDC-0941. The kinase activity of mTORC2 was then assessed as in B. The top panels are from the same gel, without differential exposure. (D) NMuMG cells were treated or not with TGF-β for the indicated times, in the presence or absence of SB431542 or LY294002. Cell lysates were subjected to immunoprecipitation using Rictor antibody, and/or immunoblotted.
S1105	LY294002 LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。	Cell,2019, 176(6):1379-1392 Nat Cell Biol,2019, 21(2):226-237 Clin Cancer Res,2019, 25(5):1639-1649	Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
S2226	Idelalisib (CAL-101, GS-1101) Idelalisib (CAL-101, GS-1101) 是选择性p110δ抑制剂，在无细胞试验中IC50为 2.5 nM；对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍，对p110δ的选择性是对 C2β，hVPS34，DNA-PK 和 mTOR的400到4000倍。	Leukemia,2019, 10.1038/s41375-019-0486-9 Am J Transplant,2019, 19(5):1305-1314 Epigenetics,2019, 1-16	293T cells were transfected with HA-tagged Fbxo45. At 48 h after transfection, cells were treated with AKT inhibitor (CAL-101; 10 uM, 4 h), cell extracts from the cytoplasm or nuclei were subjected to IP with anti-HA resin followed by western blot analysis with indicated antibodies.
S2247	Buparlisib (BKM120, NVP-BKM120) Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34，mTOR，DNAPK 的作用效果下降，而对 PI4Kβ几乎没有活性。Phase 2。	Science,2019, 364(6441) Nat Cell Biol,2019, 21(2):226-237 Nat Commun,2019, 10(1):2910	AN3CA (A) and JHUEM2 (B) cells were treated for the indicated times with DMSO, 0.3 μM BGJ398 (BGJ), 0.3 μM GDC-0941 (GDC), 0.6 μM BYL719 (BYL) and 0.6 μM BKM120 (BKM) alone or in combination. Cell lysates were immunoblotted with antibodies for phospho-AKT (Ser473), total AKT, phospho-ERK (Thr202/Tyr204), ERK2, phospho-S6 (Ser240/244), total S6, phospho-4EBP1 (Thr37/46), total 4EBP1, total PARP and cleaved PARP. Tubulin was detected as the loading control. Western blot analysis of AN3CA and JHUEM2.
S6541^New	MTX-211 MTX-211是PI3K和EGFR的双重抑制剂。
S6516^New	GNE-477 GNE-477是有效的PI3K/mTOR抑制剂，对PI3Kα的IC50值为4 nM，对mTOR的K_iapp值为21 nM。
S8693^New	Selective PI3Kδ Inhibitor 1 (compound 7n) Selective PI3Kδ Inhibitor 1 (compound 7n)是PI3Kδ抑制剂，对PI3Kδ的IC50为0.9 nM，其选择性比对其他I类PI3K亚型高1000倍以上。Selective PI3Kδ Inhibitor 1对PI3Kα/γ/β的IC50值分别为3670、1460、21300 nM。
S5818^New	acalisib (GS-9820) acalisib (GS-9820)是一种具有高度选择性的、有效的p110δ抑制剂，IC50为14 nM。它对p110δ的选择性是对其他I类PI3K酶的选择性的114-400倍，对II类和III类PI3K酶和其他PI3K相关蛋白（包括mTOR和DNA-PK）没有活性。
S8752^New	leniolisib(CDZ 173) Leniolisib(CDZ 173)是有效的选择性PI3Kδ抑制剂，对PI3Kα, PI3Kβ, PI3Kγ和PI3Kδ的IC50分别为0.244, 0.424, 2.23和0.011 μM。
S8738^New	Bimiralisib (PQR309) Bimiralisib (PQR309)是一种新型的、可渗透入大脑的PI3K/mTOR双重抑制剂，在体内外具有抗淋巴瘤活性。相对于其他PI3K相关性脂质激酶、蛋白激酶和非相关性靶点，它对PI3K/mTOR具有较高选择性。
S8560^New	Seletalisib (UCB-5857) Seletalisib是新型的PI3Kδ小分子抑制剂，IC50为12 nM。它对PI3K具有显著的选择性，相对其他I型PI3K亚型，Seletalisib对PI3Kδ的选择性高24-303倍。
S1038	PI-103 PI-103是一种多靶点 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50为 2 nM/3 nM/3 nM/15 nM，对 mTOR/DNA-PK的作用较小，IC50为30 nM/23 nM。	Mol Cancer Ther,2018, 17(6):1259-1270 Int J Oncol,2018, 52(6):2051-2060 Int J Oncol,2018, 52(3):828-840	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
S2638	NU7441 (KU-57788) NU7441 (KU-57788)是一种高度有效的，选择性DNA-PK抑制剂，在无细胞试验中IC50为14 nM，也会抑制PI3K，IC50为5 μM。它可降低NHEJ的频率，而增强Cas9介导DNA剪接后发生的同源重组修复率。	FASEB J,2019, 33(6):6778-6788 Mol Biol Rep,2019, 10.1007/s11033-019-04605-0 FEBS Open Bio,2019, 9(7):1315-1326	Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
S1169	TGX-221 TGX-221 是一种p110β-特定的抑制剂，在无细胞试验中IC50为 5 nM，作用于p110β的选择性是作用于p110α的1000倍。	Cell Metab,2019, 29(6):1400-1409 Mol Cell Proteomics,2019, 18(4):669-685 Mol Cancer Ther,2018, 17(10):2091-2099	A p110β-selective antagonist rescues increased protein synthesis in synaptic fractions from Fmr1 KO mice and in LCLs from a patient with FXS. (A–C) Treatment of synaptoneurosomes with TGX-221 (1 μmol/L, 30 min) reduces p110β-specific PI3K activity and phosphorylation of the downstream target AKT in both WT and Fmr1 KO SNS, shown by a radioactive PI3K assay and phosphoAkt- specific western blot-ting (A). (B) Quantification of PI3K activity using a competitive ELISA showed a significant reduction in PI3K activity in both genotypes after treatment [ n = 4, 2-way ANOVA, P (genotype) = 0.0086, P (treatment) = 0.0087, P (interaction) = 0.7154]. (C) Densitometric quantification of phosphoAkt-specific western blots showed a significant effect of treatment (C, n = 4, 2-way ANOVA, *P (treatment) = 0.0005, P (genotype) =0.372, P (interaction) = 0.4894).
S1268	IC-87114 IC-87114是一种选择性的PI3Kδ抑制剂，无细胞试验中IC50为0.5 μM，作用于PI3Kδ比作用于PI3Kγ和PI3Kα/β选择性分别高58和100倍。	Int J Oncol,2018, 52(3):828-840 Am J Transplant,2016, 16(9):2624-38 Cancer Cell,2015, 27(1):97-108
S2758	Wortmannin Wortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。也会抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。	Cell,2019, 176(6):1379-1392 Nat Cell Biol,2019, 21(2):226-237 Theranostics,2019, 9(15):4375-4390	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
S1118	XL147 analogue XL147 analogue是一种选择性的，可逆的I型PI3K抑制剂，作用于PI3Kα/δ/γ，无细胞试验中IC50分别为39 nM/36 nM/23 nM，对PI3Kβ作用效果稍弱。Phase 1/2。	Oncogene,2015, 10.1038/onc.2015.143 Cancer Res,2014, 74(18):5184-94 PLoS One,2014, 9(8):e105280	Breast cancer cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of XL147 for 24 hours.
S1072	ZSTK474 ZSTK474抑制I型PI3K亚型，在无细胞试验中IC50为37 nM，对PI3Kδ作用最显著。Phase 1/2。	Leukemia,2018, 32(1):159-167 J Cell Physiol,2018, 233(3):1796-1811 NAT MATER,2017, 10.1038/NMAT5024	Representative Western blot of Erk1/2, phospho-Erk1/2, Akt, phospho-Akt antibodies in BCPAP, K1 and 8505C cells treated at 4 h using IC50 doses. 1, cells untreated; 2, cells treated with RAF265; 3, cells treated with ZSTK474; 4, cells treated with SB590885; 5, cells treated with RAF265+ZSTK474; 6, cells treated with SB590885+ZSTK474.
S2814	Alpelisib (BYL719) Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。	Science,2019, 364(6441) Nat Med,2019, 25(5):838-849 Cell Rep,2019, 27(1):294-306	BYL719 induces Apoptosis in MM cells. The effect of increasing concentrations of BYL719 (0-2.5 umol/l) for 48 h on the apoptosis of MM1s cells. The effect of BYL719 on the apoptosis signalling; cleaved PARP, caspase 3, caspase 9 by Western blotting. MM, multple myeloma.
S1410	AS-605240 AS-605240选择性抑制PI3Kγ，IC50为8 nM，作用于PI3Kγ比作用于PI3Kδ/β和PI3Kα选择性分别高30和7.5倍以上。	Cell Rep,2019, 27(2):631-647 Oncol Lett,2018, 15(2):2105-2110 Cell Host Microbe,2017, 21(5):611-618	After starved in serum-free medium for 24 h, Breast cancer cells incubated with the indicated concentrations of AS-605240 for 3 h,followed by 15-minute stimolation of 100ng/ml EGF
S1205	PIK-75 HCl PIK-75 HCl是一种p110α抑制剂，IC50为5.8 nM (比作用于p110β效果强200倍)，在Ser773处功能特异性突变，也有效抑制DNA-PK，无细胞试验中IC50为2 nM。	Cancer Cell,2019, 35(5):752-766 Cell Metab,2019, 29(6):1400-1409 Mol Cell Proteomics,2019, 18(4):669-685	A549 cells were treated with DMSO or PIK-75 (200 nM) for 1 h and subsequently stimulated with izTRAIL for 24 h. Long-term survival was visualized after 7 days by crystal violet staining. One of two independent experiments is shown.
S2767	3-Methyladenine (3-MA) 3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。现配现用（加热助溶）。	Acta Neuropathol,2019, 138(1):67-84 Cell Rep,2019, 27(7):2075-2091.e5 Cell Death Differ,2019, 26(6):1077-1088	granulosa cells (GCs) with 24 h of melatonin (10 μM) treatment were rinsed in PBS, and then exposed to H2O2 (200 μM) for 2 h. The autophagy inhibitor 3-MA (10 mM), or the apoptosis inhibitor Z-VAD-FMK (50 μM) were added 1 h prior to H2O2 incubation. Cell viability was determined using the CCK-8 assay. Data represent mean ± S.E; n = 3 in each group. P < 0.05 (*P < 0.01) vs. vehicle group at 0 h. # Represents P < 0.05 (## Represents P < 0.01) vs. H2O2-only-treated cells. & Represents P > 0.05 vs. H2O2-only-treated cells. N, not significant, P > 0.05. δ Represents P < 0.05 (δδ Represents P < 0.01) vs. Z-VAD-FMK-treated cells.
S2636	A66 A66是一种有效的特异性p110α抑制剂，无细胞试验中IC50为32 nM，作用于p110α比作用于其他I类PI3K亚型选择性高100多倍。	Int J Cancer,2019, 145(3):817-829 Mol Cell Biochem,2018, 439(1-2):199-211 Cancer Immunol Res,2017, 5(8):695-709	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of A66 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S1523	Voxtalisib (SAR245409, XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue是作用于mTOR/PI3K的双重抑制剂，对p110γ作用最强，IC50为9 nM；也可抑制DNA-PK和mTOR。Phase 1/2。	Cell Rep,2015, 11(3):446-59 Mol Cancer Res,2014, 12(5):703-13 Am J Transl Res,2014, 6(5):471-493	The TMZ/XL765 combination decreases serum GH and PRL of mice bearing GH3 xenografts. A and B, After treatment with DMSO, TMZ, XL765, or the XL765/TMZ combination, the blood of the nude mice xenograft with GH3 tumor was collected and serum rat-GH and rat-PRL were measured by IRMA (TMZ/XL765 combination vs TMZ or XL765 alone: ***P <.001).
S2658	Omipalisib (GSK2126458, GSK458) Omipalisib (GSK2126458, GSK458)是一种高选择性的，有效的p110α/β/γ/δ和 mTORC1/2抑制剂，无细胞试验中K_i分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。Phase 1。	Clin Cancer Res,2019, 25(5):1639-1649 Cancer Genomics Proteomics,2018, 15(4):239-248 Cancer Lett,2017, 406:47-53
S1187	PIK-90 PIK-90是一种PI3Kα/γ/δ抑制剂，IC50分别为11 nM/18 nM/58 nM，对PI3Kβ作用效果稍弱。	Int J Oncol,2018, 52(3):828-840 Exp Mol Med,2015, 47:e143 Biochim Biophys Acta,2015, 1853(10 Pt A):2570-9	Tyr(P)^Irs1 determined in CHO^IR/Irs1 cells treated with kinase inhibitors. Cells were treated for 30 min without or with PIK-90 at concentrations increasing sequentially 2-fold between the boundaries shown in Fig. 4 before incubation with insulin (30 nM, 30 min). Cleared lysates were subject to immunoblotting with antibodies against Irs1 or Tyr(P). The bands were quantified on a Kodak Image Station 4000MM Pro, and the data were analyzed using Carestream Molecular Imaging software version 5.0.
S1462	AZD6482 AZD6482是一种PI3Kβ抑制剂，无细胞试验中IC50为10 nM，作用于PI3Kβ比作用于PI3Kδ， PI3Kα和PI3Kγ选择性分别高8，87和109倍。Phase 1。	Mol Cancer Res,2017, 10.1158/1541-7786.MCR-16-0183 Breast Cancer Res,2016, 10.1186/s13058-016-0697-1 Thromb Haemost,2016, 115(6):1138-46	Cells treated with either control or INPP4B siRNA and following a 1-hour treatment with either DMSO or 1 mmol/L inhibitor; pPRAS40T246 and total PRAS40 were run on a separate blot for which the bottom Ku-86 panel is the loading control(pan-PI3Ki: GDC-0941, PI3K-ai: BYL719,PI3K-bi: AZD6482)
S2743	PF-04691502 PF-04691502是一种ATP竞争性的PI3K(α/β/δ/γ)/mTOR双重抑制剂，在无细胞试验中K_i为1.8 nM/2.1 nM/1.6 nM/1.9 nM和16 nM，对Vps34， AKT， PDK1， p70S6K， MEK， ERK， p38 和 JNK 几乎没有作用活性。Phase 2。	Onco Targets ,2018, 11:943-953 Clin Cancer Res,2016, 10.1158/1078-0432.CCR-16-1971 Int J Oncol,2016, 48(1):253-60	BMDMs from WT animals were treated with different concentrations of PI3K inhibitors (500 nmol/L PF4691502, PI-103, BKM120 and 25 μmol/L SF1126) followed by hypoxia for 4 hours for Western blots. These macrophages were either used for lysate preparation (nuclear extracts for HIFα or WCE for pAKT and AKT) and Western blot analysis.
S2696	Apitolisib (GDC-0980, RG7422) Apitolisib (GDC-0980, RG7422)是一种有效的，I型PI3K抑制剂，作用于PI3Kα/β/δ/γ，无细胞试验中IC50分别为5 nM/27 nM/7 nM/14 nM，也是mTOR抑制剂，无细胞试验中K_i为17 nM，比作用于其他PIKK家族激酶选择性高。Phase 2。	Cell Death Dis,2019, 10(3):231 Leukemia,2018, 10.1038/s41375-018-0012-5 Oncogene,2016, 35(38):5070-7	Immunoblots from AR + TNBC cell lines treated with either CDX (25 uM), GDC-0941 (300 nM) or GDC0980 (100 nM) as single agents or CDX in combination with either GDC-0941 or GDC-0980 for 48 h analyzed for AR, p-AKT, AKT, p-S6, S6 and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) protein.
S1360	GSK1059615 GSK1059615是一种PI3Kα/β/δ/γ (可逆的)和mTOR的双重抑制剂，IC50分别为0.4 nM/0.6 nM/2 nM/5 nM和12 nM。Phase 1。	Cell Rep,2019, 27(3):820-834 Int J Oncol,2018, 52(3):828-840 BMC Cancer,2017, 17(1):199	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of GSK1059615 for 24 hours.
S7028	Duvelisib (IPI-145, INK1197) Duvelisib (IPI-145, INK1197) 是一种新型选择性PI3K δ/γ抑制剂，在无细胞试验中K_i和IC50分别为 23 pM/243 pM 和 1 nM/50 nM，对 PI3K δ/γ 的选择性比对其它蛋白激酶高。Phase 3。	Leukemia,2019, 10.1038/s41375-019-0486-9 Cell Rep,2019, 27(2):631-647 Lab Invest,2019, 99(5):648-658	PI3K inhibitor IPI-145 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range.
S2628	Gedatolisib (PF-05212384, PKI-587) Gedatolisib (PF-05212384, PKI-587)是一种高度有效的，双重PI3Kα，PI3Kγ和mTOR抑制剂，无细胞试验中IC50分别为0.4 nM， 5.4 nM和1.6 nM。Phase 2。	Mol Cancer Ther,2016, 15(3):412-20 Clin Cancer Res,2015, 21(12):2792-801 Cell Rep,2015, 11(3):446-59	PI3K inhibitors promote apoptosis in checkpoint-defective cell lines. Two checkpoint-functional (A2058, D28) and three defective (HT144, D20, SKMel13) melanoma cell lines growth as tumour spheres as in Figure 4B were either untreated or treated with 5 uM PF-05212384 for 72 h, harvested and immunoblotted for pAkt Ser473.
S1352	TG100-115 TG100-115是一种PI3Kγ/δ抑制剂，IC50为83 nM/235 nM，对PI3Kα/β几乎没有抑制效果。Phase 1/2。	Int J Oncol,2018, 52(3):828-840 Biochim Biophys Acta,2017, 1861(4):947-957 Biochim Biophys Acta,2017, 1861(4):947-957	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
S2671	AS-252424 AS-252424是一种新型，有效的PI3Kγ抑制剂，无细胞试验中IC50为30 nM，作用于PI3Kγ比作用于PI3Kα选择性高30倍，对PI3Kδ/β具有低的抑制活性。	Inflammation,2017, 40(2):435-441 Immunol Res,2015, 10.1007/s12026-015-8648-y Blood,2014, 123(2):239-51	Effects of AS252424 on KL-induced cPLA 2 phosphorylation in BMMCs. BMMCs were pre-incubated with AS252424 for 1 h followed by stimulation with KL for 15 min. The phosphorylation of cPLA 2 was evaluated via immunoblot analysis. Results are representative of three independent experiments.P<0.05, P<0.01, **P<0.001 and ### P<0.001, compared with BMMCs with KL induction but without pretreatment by AS252424.
S2749	BGT226 maleate (NVP-BGT226 maleate) BGT226 (NVP-BGT226)是一种新型I型PI3K/mTOR抑制剂，作用于PI3Kα/β/γ，IC50为4 nM/63 nM/38 nM。Phase 1/2。	Oncotarget,2016, 7(48):79842-79853 Mol Cancer Ther,2015, 14(8):1928-38 Oncotarget,2015, 6(19):17147-60	IGROV1-R10 cells were treated with BGT266(250nM) for 8 h.The effect of BGT226 on PI3K/Akt/mTOR pathway activation (A) and on expression of Mcl-1 and Bim (B).
S2759	CUDC-907 CUDC-907是一种PI3K和HDAC双重抑制剂，作用于PI3Kα和HDAC1/2/3/10，IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。Phase 1。	EBioMedicine,2018, 28:80-89 J Cell Mol Med,2018, 10.1111/jcmm.13935 Biochem Pharmacol,2018, 148:13-26	Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 for uninduced cells (a), adipocyteinduced hMSCs exposed to the vehicle control (b) or CUDC-907-treated cells (500 nM) (c). Nile red staining (d and e) on day 7 of post-adipocytic induction in hMSCs and after exposure to CUDC-907. Images were captured at ×20 magnification using the FLoid Cell Imaging Station. The level of Nile red staining was quantified using the Molecular Devices M5 Microplate Reader (f). Data are presented as mean ± S.E (n = 16) from three independent experiments, ***P <0.0005.
S2227	PIK-294 PIK-294是一种高度选择性p110δ抑制剂，IC50为10 nM，作用于PI3Kα/β/γ效果分别低1000，49和16倍。	Cell Metab,2019, 29(6):1400-1409 Mol Cell Biol,2012, 32(12):2268-78	After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PIK-294 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
S2681	AS-604850 AS-604850是一种选择性的，ATP竞争性的PI3Kγ抑制剂，IC50为250 nM，作用于PI3Kγ比作用于PI3Kδ/β选择性高80倍以上，作用于PI3Kγ比作用于PI3Kα选择性高18倍。	Nature,2017, 542(7642):489-493 J Biol Chem,2014, 289(46):32109-20	Representative blots of activated Rac1 and total Rac1 in response to high glucose shown in cells treated overnight with either DMSO or AS604850 (1 umol/liter).
S8002	GSK2636771 GSK2636771是一种口服生物有效的PI3Kβ选择性抑制剂，其对PI3Kβ的选择性比对PI3Kα/PI3Kγ高900倍以上，比对PI3Kδ的选择性大10倍以上。对PTEN缺失细胞系敏感。	Cell Signal,2019, 53:122-131 Cancer,2018, 124(18):3693-3705 FASEB J,2018, 10.1096/fj.201800183R	Cells were treated as indicated. Medium and drug were refreshed every 2 to 3 days, and protein lysates were analyzed as above.
S2802	Copanlisib (BAY 80-6946) Copanlisib (BAY 80-6946)是一个高效的泛I型 PI3K抑制剂，其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3。	Cell Death Discov,2019, 5:86 Nature,2018, 560(7719):499-503 Biomed Res Int,2018, 2018:1023490	The compounds BAY80-6946 and TG100713, which are respectively an alpha/beta- and a pan-isoforms inhibitors, demonstrated a very good ability to block Jurkat E6.1 proliferation with an IC50 slightly higher than 1 mM.
S2699	CH5132799 CH5132799抑制I型PI3Ks，尤其是PI3Kα，IC50为14 nM；对PI3Kβδγ作用效果稍弱，对PIK3CA突变型细胞系敏感。Phase 1。	Biochimie,2014, 105:182-91 Am J Transl Res,2014, 6(5):471-493	Effect of selected compounds on MLC phosphorylation induced by 2-AG. Washed platelets (1.0 x 10⁹ platelets/mL) were preincubated at 37 ℃ for 10 min with saline or 20 uM LY294002 (L), 10 uM CH5132799 (C), 10 uM TGX221 (T), 10 uM MK2206 (M), 20 uM Y27632 (Y), 1 uM PIK-75 (P), 1 U/mL apyrase (AP), 5 uM AS252424 (AS), 1 uM IC87114 (IC) and then stimulated for 30 s with 10 uM 2-AG. At the end of incubation suitable aliquots were immunoblotted with anti-p-MLC (thr18/ser19) as detailed in Methods. Blot is representative of four independent experiments.
S2682	CAY10505 CAY10505是AS-252424的羟基化合物，是一种PI3Kγ抑制剂，IC50为30 nM.	Br J Haematol,2014, 166(4):529-39	(D) Box plots showing the results of primary MM cell treatment (n = 22; in co-culture with BMSCs) with PI3K inhibitors (10 umol/l each). BYL-719 exerted the strongest anti-myeloma effects of TGX-221, CAY10505 or CAL-101. The mean survival value is indicated by a horizontal bar and the end of the whiskers show the values of the most sensitive and most resistant sample, respectively. (E) Treatment of PBMCs (n = 5) for 5 d with PI3K isoform-specific inhibitors (10 umol/l each).
S2207	PIK-293 PIK-293是一种PI3K抑制剂，最有效作用于PI3Kδ，IC50为0.24 μM，作用于PI3Kα/β/γ效果分别低500，100和50倍。		After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PIK-293 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
S2739	PKI-402 PKI-402是一种有效的，pan-PI3K/mTOR双重抑制剂，靶向作用于PI3Kα/β/γ/δ和mTOR，IC50分别为2 nM/7 nM/16 nM/14 nM和3 nM，也有效作用于PI3Kα突变型E545K和H1047R。	Cancer Lett,2019, 443:135-144
S2870	TG100713 TG100713是一种pan-PI3K抑制剂，作用于PI3Kγ， PI3Kδ， PI3Kα和PI3Kβ，IC50分别为50 nM， 24 nM， 165 nM和215 nM。	MedChemComm,2013, 10.1039/c3md00301a	The compounds BAY80-6946 and TG100713, which are respectively an alpha/beta- and a pan-isoforms inhibitors, demonstrated a very good ability to block Jurkat E6.1 proliferation with an IC50 slightly higher than 1 mM.
S7016	VS-5584 (SB2343) VS-5584 (SB2343)是一种有效的，选择性，PI3K/mTOR双重抑制剂，抑制mTOR和PI3Kα/β/δ/γ，IC50分别为3.4 nM和2.6-21 nM。Phase 1。	Biomed Pharmacother,2018, 428-437 Platelets,2018, 29(3):277-287 Cell Physiol Biochem,2018, 47(2):680-693	Effect of VS-5584 on platelet adhesion. A-F: WP (A, B) and PRP (D, E) were treated with DMSO as vehicle (A, D; n = 3) or with 20 nM (B; n = 3) and 20 μM (E; n = 3) of VS-5584 and seeded on siliconized coverslips for the quantitative analysis of WP (C) and PRP adhesion (F). Scale bars: A, B, D, E = 50 μm; Data are given in % of vehicle. Mean ± SEM. p < 0.05 vs. vehicle. G, H: Representative images of WP treated with vehicle (G) or 20 nM of VS-5584 (H). The number of non-spread cells (arrows) is higher in VS-5584-treated WP. Scale bars: 20 μm. I: Quantification of spread platelets based on their morphology. Data are given in % of vehicle. Mean ± SEM. p < 0.05 vs. vehicle.
S7103	Taselisib (GDC 0032) Taselisib (GDC 0032)是一种有效，下一代的β亚型PI3K抑制剂，作用于PI3Kα/δ/γ， IC50分别为0.29 nM/0.12 nM/0.97nM，比作用于PI3Kβ选择性高10倍以上。	Science,2019, 364(6441) Cell Rep,2019, 27(1):294-306 Anal Biochem,2018, 547:66-76
S7018	CZC24832 CZC24832是第一个PI3Kγ选择性抑制剂，IC50为27 nM，比作用于PI3Kβ选择性高10倍，比作用于PI3Kα和PI3Kδ选择性高100倍以上。	Leukemia,2018, 32(9):1958-1969 Sci Rep,2018, 8(1):5558 Mol Cancer Ther,2018, 17(5):1090-1100	(c) MM primary cells were treated with idelalisib (1 μm), CZC24832 (1 μm) and duvelisib (1 μm) for 72 h and then assessed for apoptosis by PI/Annexin V staining (n=4).
S7813	AMG319 AMG319是一种有效的选择性PI3Kδ抑制剂，IC50为18 nM，选择性比作用于其他PI3Ks高47倍多。Phase 2。
S7938	GSK2292767 GSK2292767是一种有效的、选择性的PI3Kδ抑制剂。
S8163	GDC-0084 GDC-0084是一种能透过血脑屏障的PI3K和mTOR的抑制剂，对PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ 和mTOR的Kiapp分别为2 nM, 46 nM, 3 nM, 10 nM和70 nM。
S8157	GDC-0326 GDC-0326是一种有效的、选择性的PI3Kα抑制剂，Ki值为0.2 nM。在酶活性实验中，对PI3Kα的选择性显著高于其它I类亚型。	Microb Cell,2018, ;5(12):545-554
S7356	HS-173 HS-173 是强效的PI3Kα抑制剂，其IC50为0.8 nM。	Sci Rep,2018, 8(1):5558 Cancer Cell Int,2017, 10.1186/s12935-017-0396-8 Cancer Cell Int,2017, 17:112	b, d Serum-deprived MG-63 (b) and U20S cells (d) were pre-treated with 1 nmol/L HS-173 (PI3Kα inhibitor), 10 nmol/L TGX-221 (PI3Kβ inhibitor), 10 nmol/L CZC24832 (PI3Kγ inhibitor) and 10 nmol/L CAL-101 (PI3Kδ inhibitor) for 1 h, then were incubated with 100 ng/mL Wnt5a and harvested at 30 min after the start of Wnt5a treatment. Data were presented as mean ± SD of 3 determinations. The relative RhoA activity was normalized to the average value of each inhibitor-untreated group
S8589	SF2523 SF2523是一种有效的、具有高度选择性的PI3K抑制剂，对PI3Kα, PI3Kγ, DNA-PK, BRD4 和 mTOR的IC50分别为34 nM, 158 nM, 9 nM, 241 nM 和 280 nM。
S8581	Serabelisib (INK-1117,MLN-1117,TAK-117) Serabelisib (INK-1117,MLN-1117,TAK-117)是一种有效的、选择性的，可用于口服的PI3Kα抑制剂，IC50为21 nM。对PI3Kα的选择性比对其他I类PI3K家族成员高100倍以上。
S8330	IPI-549 IPI-549是PI3K-γ的有效抑制剂，选择性是对其他脂质和蛋白激酶的100倍以上。生化IC50为16 nM。
S2391	Quercetin Quercetin是蔬菜水果和白酒中的天然黄酮类化合物，是一种体外重组Sirt1蛋白的激活剂同时也是PI3K抑制剂，IC50为2.4 – 5.4 μM。	Front Cell Neurosci,2019, 13:316 Clin Cancer Res,2018, 10.1158/1078-0432 Mol Nutr Food Res,2017, 61(4)	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S8456	VPS34 inhibitor 1 (Compound 19, PIK-III analogue) VPS34 inhibitor 1 (Compound 19, PIK-III analogue)是有效的、选择性的VPS34抑制剂，IC50为15 nM。	Oncotarget,2017, 8(24):38099-38112	Confirmation of selective growth inhibition using VPS34-IN1 inhibitor. Proliferation of Tsc2+/+ and Tsc2-/- MEFs treated with vehicle control (DMSO), CQ (5 uM), VPS34-IN1 (500 nM) or the combination for 72 hours (crystal violet staining). Two sample t-test was carried out between CQ and SAR405 and each drug alone. Results are representative of three independent experiments. Bar graph represent means ±SD.
S7646	Voxtalisib (XL765, SAR245409) Voxtalisib (SAR245409, XL765)是作用于mTOR/PI3K的双重抑制剂，对p110γ作用最强，IC50为9 nM；也可抑制DNA-PK和mTOR。Phase 1/2。	Biomed Pharmacother,2018, 103:1069-1078 Nat Neurosci,2017, 20(8):1074-1084 Int J Oncol,2015, 47(3):1143-59	HL60, HL60/ADR, K562 and K562/A02 cells pretreated with various concentrations of Voxtalisib (0, 0.625, 1.25, 2.5, 5 and 10 μM) for 48 h were harvested for western blot. The levels of cyclin D1, p27, and p-pRb in the nuclei were determined.
S8596	Autophinib Autophinib是有效的自噬 (autophagy)抑制剂，在饥饿诱导的自噬试验和rapamycin诱导的自噬试验中，其IC50分别为90 nM和40 nM。它还是Vps34的抑制剂，IC50为19 nM。	Cell Rep,2019, 27(12):3413-3421
S7798	GNE-317 GNE-317 是一种有效的，大脑渗透性 PI3K 抑制剂。
S8672	Tenalisib (RP6530) Tenalisib (RP6530)是一种有效的、选择性的PI3Kδ/γ抑制剂，对PI3Kδ和PI3Kγ的IC50值分别为24.5 nM和33.2 nM。它对δ/γ的选择性比对α和β亚型高300倍和100倍以上。
S8194	umbralisib (TGR-1202) TGR-1202是一种新型的PI3Kδ抑制剂，在酶学研究中和在细胞研究中，其抑制PI3Kδ活性的IC50和EC50分别为22.2 nM和24.3 nM。
S7937	Nemiralisib (GSK2269557) Nemiralisib，又名GSK-2269557，是有效的、选择性的PI3Kδ抑制剂（pKi=9.9）。
S8322	LY3023414 LY3023414是一种口服的ATP竞争性抑制剂，抑制I类PI3K亚型、mTOR和DNA-PK。		The structure and formula weight of LY3023414 were presented (A). Established human glioma cells (U251MG and A172 lines), primary human astrocytes (“Astrocytes”) or primary human glioma cells [three lines, “Glioma (L1/2/3)”], were either left untreated (“Ctrl”) or treated with LY3023414 at 1-1000 nM, cells were further cultured for indicated time; Cell survival was tested (B, C, and E) (n=5). Cell proliferation was also tested by the BrdU ELISA assay (D and F) (n=5). *p < 0.05 vs. “Ctrl”. Experiments in this figure were repeated three times.
S7980	VPS34-IN1 Vps34-IN1 是Vps34的抑制剂，在体外实验中所测得的IC50为25 nM, 对1型和2型 PI3K没有显著抑制作用。	Oncotarget,2017, 8(24):38099-38112	C. Lysosomal and endosomal inhibition selectively targets Tsc2−/− MEFs. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), Vps34 inhibitor (SAR405; 1uM) or the combination for 72 hours (crystal violet staining). D. Confirmation of selective growth inhibition using VPS34-IN1 inhibitor. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), VPS34-IN1 (500nM) or the combination for 72 hours (crystal violet staining). Two-sample t-test was carried out between CQ and SAR405 and each drug alone. Results are representative of three independent experiments. Bar graph represent means ±SD.
S8696	2-D08 2-D08是一种具有细胞透性的蛋白类泛素化（protein sumoylation）抑制剂。它还能抑制Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。
S7335	IPI-3063 IPI-3063是有效的、选择性的p110δ抑制剂，在无细胞实验中，IC50为2.5 ± 1.2 nM。其对其他I型PI3K亚型如p110α, p110β, p110γ的IC50s至少高400倍。
S7682	SAR405 SAR405是一种低分子量的Vps34抑制剂（Kd=1.5 nM），具有高选择性，在浓度高达10 μM时，对I类和Ⅱ类PI3Ks及mTOR没有活性。	Urol Oncol,2018, 36(4):160.e1-160.e13	RT-112 and RT-112 (CisPt-R) cells were treated with cisplatin, SAR405, and a combination of both in absence and presence of QVD (10 µM). Again, the concentrations used were the IC50 or half IC50 values for RT-112 (CisPt-R) and RT-112, respectively. After 48 hours, the cells were lysed, and cleared cellular lysates were subjected to SDS-PAGE and immunoblotting for PARP, caspase-3 (Casp3), and Actin. One representative immunoblot is shown.
S7683	PIK-III PIK-III, 一种选择性VPS34酶活性的抑制剂，抑制细胞自噬以及LC3的重新脂化，稳定自噬底物。其对VPS34和 PI(3)Kδ的IC50值分别为0.018 μM和1.2 μM。	Cancer Lett,2018, 435:32-43 Mol Biosyst,2017, 13(10):1993-2005	LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm
S7623	PI-3065 PI-3065是一种选择性p110δ抑制剂，IC50为15 nM,选择性比其他PI3K家族成员高出70多倍。	Leukemia,2019, 33(6):1427-1438
S7645	Pilaralisib (XL147) Pilaralisib (XL147)是一种选择性的可逆I型PI3K抑制剂，作用于PI3Kα/δ/γ，在无细胞试验中IC50为 39 nM/36 nM/23 nM，对PI3Kβ作用较低。Phase 1/2。	Cell Rep,2019, 27(2):631-647 Neoplasia,2019, 21(6):615-626 J Cell Biochem,2018, 119(8):6398-6407	I. OMI index decreases in BT474 organoids treated with single and combination therapies at 24 hr. J. OMI index of BT474 organoids treated for 72hr. Red bars denote p<0.05 for treated organoids vs. control. H:trastuzumab (anti-HER2); P:paclitaxel (chemotherapy); XL147 (X).
S7966	AZD8835 AZD8835是一种新型的PI3Kα和PI3Kδ混合型抑制剂，IC50分别为6.2 nM和5.7 nM。对PI3Kβ和PI3Kγ同样具有选择性，IC50分别为431 nM和90 nM。
S8132	Deguelin Deguelin，一种从植物中分离出来的天然产物，是PI3K/Akt的抑制剂。
S7675	PF-4989216 PF-4989216 是一种有效的选择性PI3K抑制剂，对p110α，p110β，p110γ，p110δ，和 VPS34的 IC50 分别为 2 nM，142 nM，65 nM，1 nM，和 110 nM。
S7694	AZD8186 AZD8186是一种有效的选择性PI3Kβ和PI3Kδ抑制剂，IC50分别为 4 nM 和 12 nM。Phase 1。	EBioMedicine,2018, 28:80-89

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S7865	740 Y-P (PDGFR 740Y-P) 740 Y-P是具有细胞可透过性的PI3K磷酸肽激活剂。	J Recept Signal Transduct Res, 2019, 39(1):80-86 Neurochem Res, 2018, 43(6):1210-1226

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