HSP (HSP90)

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

HSP (HSP90)产品

所有产品(36) HSP (HSP90)抑制剂(27) HSP (HSP90)激活剂(5) HSP (HSP90)调节剂(3)

目录号	产品描述	文献引用	实验数据
S1141	Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。	Nat Commun, 2020, 29;11(1):2086 Cancers (Basel), 2020, 7;12(4) Mol Cell Biol, 2020,	SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
S1069	Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定，从而导致抑制生长、自噬和凋亡。Phase 2。	Cancer Cell, 2020, 37(3):371-386 Nat Commun, 2020, 11(1):562 Genome Med, 2020, 18;12(1):17
S1142	Alvespimycin (17-DMAG) HCl Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。	Nat Commun, 2020, 22;11(1):1935 Aging Cell, 2020, e13269 Cancers (Basel), 2020, 12(11)E3335
S1159	Ganetespib (STA-9090) Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cancer Discov, 2020, 10(5):674-687	Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.
S1175	BIIB021 BIIB021 (CNF2024)是一种口服有效的，全部人工合成的，小分子HSP90抑制剂，K_i和EC50分别为1.7 nM和38 nM。Phase 2.	SLAS Technol, 2019, 24(1):28-40 ACS Chem Neurosci, 2019, 10(6):2890-2902 Mol Syst Biol, 2018, 14(3):e7858
S1163	Onalespib (AT13387) Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。	Eur J Nucl Med Mol Imaging, 2020, 47(4):980-990 Sci Rep, 2020, 3;10(1):5923 Cell Biochem Funct, 2020, 10.1002/cbf.3566	IC50 determinations of compound S1 and S13 on heat shock poteins ATPase activity using ADP fluorescence assay. (A) inhibition of HSP70 (B) inhibition of HSP90 The test compounds were diluted from mother plates (10 mM in 100% (v/v) DMSO) into series of concentration (in 2.0% (v/v) DMSO). AT13387 and 17-DMAG were used as positive controls in each assay. Data were performed in triplicate and analyzed by GraphPad.Prism.
S1498	NVP-BEP800 NVP-BEP800 (VER82576) 是一种新型的，全部人工合成的HSP90β抑制剂，IC50为58 nM，比作用于Hsp90家族成员Grp94和Trap-1选择性高70倍以上。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Theranostics, 2020, 10(18):8415-8429	Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800).
S2713	Geldanamycin Geldanamycin (NSC 122750) 是一种天然的HSP90抑制剂，K_d为1.2 μM，特异性干扰糖皮质激素受体(GR)/HSP联合。Geldanamycin 通过减少宿主的炎症反应来减轻病毒感染引起的ALI(急性肺损伤)/ARDS(急性呼吸窘迫综合征)。	Anal Chem, 2020, 92(1):1363-1371 Anal Chem, 2020, 10.1021/acs.analchem.0c02756 Cell Biol Toxicol, 2020,	Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
S2639	SNX-2112 (PF-04928473) SNX-2112 (PF-04928473)选择性结合到HSP90α和HSP90β的ATP结合袋中，K_a分别为30 nM和30 nM，比17-AAG更有效。	PLoS Negl Trop Dis, 2020, 17;14(4):e0008224 Onco Targets Ther, 2020, 13:7907-7919 Nat Commun, 2019, 10(1):402
S2656	PF-04929113 (SNX-5422) PF-04929113 (SNX-5422)是一种有效的，选择性的HSP90抑制剂，K_d为41 nM，且诱导Her-2降解，IC50为37 nM。Phase 1/2。	ACS Chem Neurosci, 2019, 10(6):2890-2902 Endocrine, 2016, 51(2):274-82 Antimicrob Agents Chemother, 2014, 58(7):4138-44	Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.
S2685	KW-2478 KW-2478是一种非Ansamycin的HSP90抑制剂，IC50为3.8 nM。Phase 1。	Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
S7122	XL888 XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。Phase 1	Oncotarget, 2016, 7(31):49597-49610 Clin Cancer Res, 2012, 18(9):2502-14	B, XL888 (1 mmol/L, 144 hours) is effective at blocking the growth and survival of vemurafenib-resistant melanoma cell lines grown as 3D collagen-implanted spheroids. Staining shows cell viability, in which green corresponds to live cells and red: dead cells. Magnification×4.
S2930	Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ) 是一种特异性的p53抑制剂，通过降低其与Bcl-xL和Bcl-2的亲和力而发挥作用，也抑制HSP70功能和细胞自噬。	Radiat Res, 2020, 193(2):119-129 Clin Transl Med, 2020, 10.1002/ctm2.41 Theranostics, 2019, 9(2):554-572	Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
S7282	NMS-E973 NMS-E973 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。	Immunity, 2020, 52(2):328-341 Mol Cancer, 2020, 19(1):112 Theranostics, 2020, 10(18):8415-8429	(D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.
S8039	PU-H71 PU-H71 (NSC 750424)是有效的选择性HSP90抑制剂，IC50为51 nM。	Cancers (Basel), 2020, 7;12(4) Mol Cell Biol, 2020, Theranostics, 2019, 9(2):554-572	Effects of low-level HSP90 inhibition (by ganetespib, 2-5 nM; PU-H71, 40-70 nM) or febrile-range temperature (39 ℃) on HSP70 and HSP90 protein levels in FANCA wild-type cells. High-level HSP90 inhibition (ganetespib, 25 nM; PU-H71, 300 nM) as well as proteotoxic proteasomal inhibition (MG132, 2.5 mM) induced the expression of HSP70. Constitutive (upper band: C) and inducible forms (lower band: I) of HSP70 are indicated. HSP90 levels are shown for comparison.
S5369	Ethoxyquin Ethoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative.
S8365	Apoptozole Apoptozole (Apoptosis Activator VII) 是热激蛋白HSP70和Hsc70的抑制剂，与HSP70和Hsc70的Kd值分别为0.14 μM和0.21 μM。它能够诱导caspase依赖性的凋亡反应。	Nat Commun, 2018, 9(1):4700 Platelets, 2018, 29(6):610-621	Representative images of platelets preincubated with FITC-conjugated CD41 before treated with negative control, pitstop 2, dynasore, A23, or apoptozole spreading on immobilized Fg for 10, 30, and 60 minutes, respectively. Images were taken under oil immersion with magnification × 100. Scale bar, 5 μm.
S8402	KRIBB11 KRIBB11 抑制热激诱导的荧光素酶活性，IC50为1.2 μM。它是转录因子热休克因子1(HSF1)的抑制剂。KRIBB11 可诱导生长阻滞和凋亡。	FASEB J, 2020, 34(6):7927-7940 Cancer Discov, 2020, CD-20-0160 Theranostics, 2019, 9(10):2999-3013
S7750	KNK437 KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。	Biosci Rep, 2020, 40(3) Br J Haematol, 2013, 161(5):667-76 Oncol Rep, 2012, 28(6):1953-8	Western blots of lysates from BaF3 JAK2 V617F cells.
S7458	VER-49009 VER-49009 (CCT0129397) 是一种强效的HSP90抑制剂，其IC50为 47 nM。
S7716	TAS-116 TAS-116是一种新型的HSP90小分子抑制剂，HSP90α和HSP90β的Ki值分别为34.7 nmol/L和21.3 nmol/L。TAS-11并不抑制其他ATP酶，如HSP70(IC50 >200 μmol/L)。
S7340	CH5138303 CH5138303 是口服有效的Hsp90抑制剂，其K_d为 0.48 nM。
S7459	VER-50589 VER-50589 是强效的HSP90抑制剂，对HSP90β的IC50为21 nM。	PLoS Negl Trop Dis, 2014, 8(2):e2699
S3604	Triptolide (PG490) Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂，抑制NF-κB转录活性，破坏p65/CBP的相互作用，减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。	Cell Commun Signal, 2020, 18(1):30 J Cell Physiol, 2020, 4 Front Oncol, 2020, 10;10:331	Spironolactone (sp.) and triptolide inhibit NER in myeloma cells. RPMI8226 cells were incubated with dimethyl sulfoxide (DMSO), spironolactone (10 μm) or triptolide (1 μm) for 6 h before NER evaluation. The figure represents the persistence of DNA-damage signal 150 min after exposure to UV (AFU: arbitrary fluorescent unit). Figure 4a shows representative merged pictures of DAPI and DDB2 proteo-probe signal (b).
S7751	VER155008 VER155008 (C07)是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。VER155008 可抑制自噬并导致HSP90客户蛋白水平降低。	Cancer Cell, 2020, 37(3):371-386 Immunity, 2020, 52(2):328-341 Virology, 2020, 553:70-80	(D) Microglial cultures treated with 300 μM H2O2 alone or 100 μM SNAP plus 300 μM H2O2 for 24 h in the absence or presence of a chemical inhibitor (20 μM VER-155008 or 20 μM SnPP) were subjected to the determination of cell viability (MTT reduction assay). ∗p < 0.05 vs. H2O2 (300 μM) alone. +p < 0.05 vs. SNAP (100 μM) plus H2O2 (300 μM).
S6721	JG98 JG-98 是 Hsp70 的变构抑制剂，它与Hsp70家族成员保守的深袋紧密结合。JG-98 可诱导经典的凋亡特征，包括与程序性细胞死亡和膜联蛋白染色阳性相符的形态变化。JG-98 具有抗癌的活性。
S7097	HSP990 (NVP-HSP990) HSP990 (NVP-HSP990) 是一种新型有效的选择性 HSP90抑制剂，对HSP90α/β的IC50分别为0.6 nM和0.8 nM。NVP-HSP990可诱导细胞周期阻滞和凋亡。	Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669 Theranostics, 2020, 10(18):8415-8429 Mol Pharm, 2019, 16(5):2069-2082	Expression of CD24 and CD44 in HSP90 inhibitor‐treated, shRNA‐transduced HCC1937 cells was analyzed by flow cytometry.
S0279^New	Dimethylenastron Dimethylenastron 是一种有效的、特异性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制剂，其IC50值为200 nM。Dimethylenastron 可诱导人多发性骨髓瘤细胞的有丝分裂停滞和凋亡并上调 Hsp70 的表达。
S0294^New	HSF1A HSF1A 是一种可透过细胞的 heat shock transcription factor 1 (HSF1) 的激活剂。HSF1A 可保护细胞免受压力诱导的凋亡，结合TRiC亚基并抑制TRiC活性，而不会干扰ATP水解。
S1972	Tamoxifen Citrate Tamoxifen Citrate (ICI 46474) 是一种雌激素受体 estrogen receptor 调节剂 (SERM)，通过竞争性抑制雌激素结合发挥作用。Tamoxifen Citrate 也是一种有效的 Hsp90 激活剂，可增强Hsp90分子伴侣ATPase的活性。Tamoxifen 可诱导凋亡与自噬。	Acta Biomater, 2020, S1742-7061(20)30695-4 Molecules, 2020, 25(15)E3355 Molecules, 2020, 25(20)E4606	Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells.
S6568	ML346 ML346是Hsp70激活剂，是一种新型的蛋白质稳定状态调节剂。
S1238	Tamoxifen Tamoxifen (ICI 46474) 作用于乳腺组织，是一种雌激素受体estrogen receptor调节剂 (SERM)。Tamoxifen可增强Hsp90分子伴侣ATPase的活性。Tamoxifen可诱导凋亡。	Cell, 2020, S0092-8674(20)31394-5 Aging Dis, 2020, 9;11(3):523-535 Bone, 2020, 130:115123	E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01.
S1052	Elesclomol (STA-4783) Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。Phase 3。	Nat Commun, 2020, 15;11(1):2423 EBioMedicine, 2020, 54:102715 Cancers (Basel), 2020, 12(6):E1645
S8305	TRC051384 TRC051384是heat shock protein 70 (HSP70)的诱导物，同时也是有效的抗炎药。
S8299	HA15 HA15是特异靶向BiP/GRP78/HSPA5的小分子。在所检测的黑色素瘤细胞中具有抗肿瘤活性，包括从病人中分离得到的细胞和对BRAF抑制剂具有耐药性的细胞。	Am J Cancer Res, 2020, 10(8):2621-2634 J Pharm Biomed Anal, 2020, 185:113230 Cell Death Dis, 2019, 10(9):651	SP cells in inhibitor-treated, shRNA-transduced HCC1937 cells analyzed by flow cytometry using Hoechst 33342 dye. Data are shown as mean±SD. **P<.0001, P<.001, P<.01, P<.05.
S5006	Teprenone Teprenone，也被称作tetraprenylacetone或geranylgeranylacetone，是一种抗溃疡药，在临床上用于治疗胃炎。

目录号	产品描述	文献引用	实验数据
S1141	Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。	Nat Commun,2020, 29;11(1):2086 Cancers (Basel),2020, 7;12(4) Mol Cell Biol,2020,	SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
S1069	Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定，从而导致抑制生长、自噬和凋亡。Phase 2。	Cancer Cell,2020, 37(3):371-386 Nat Commun,2020, 11(1):562 Genome Med,2020, 18;12(1):17
S1142	Alvespimycin (17-DMAG) HCl Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。	Nat Commun,2020, 22;11(1):1935 Aging Cell,2020, e13269 Cancers (Basel),2020, 12(11)E3335
S1159	Ganetespib (STA-9090) Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 Cancer Discov,2020, 10(5):674-687	Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.
S1175	BIIB021 BIIB021 (CNF2024)是一种口服有效的，全部人工合成的，小分子HSP90抑制剂，K_i和EC50分别为1.7 nM和38 nM。Phase 2.	SLAS Technol,2019, 24(1):28-40 ACS Chem Neurosci,2019, 10(6):2890-2902 Mol Syst Biol,2018, 14(3):e7858
S1163	Onalespib (AT13387) Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。	Eur J Nucl Med Mol Imaging,2020, 47(4):980-990 Sci Rep,2020, 3;10(1):5923 Cell Biochem Funct,2020, 10.1002/cbf.3566	IC50 determinations of compound S1 and S13 on heat shock poteins ATPase activity using ADP fluorescence assay. (A) inhibition of HSP70 (B) inhibition of HSP90 The test compounds were diluted from mother plates (10 mM in 100% (v/v) DMSO) into series of concentration (in 2.0% (v/v) DMSO). AT13387 and 17-DMAG were used as positive controls in each assay. Data were performed in triplicate and analyzed by GraphPad.Prism.
S1498	NVP-BEP800 NVP-BEP800 (VER82576) 是一种新型的，全部人工合成的HSP90β抑制剂，IC50为58 nM，比作用于Hsp90家族成员Grp94和Trap-1选择性高70倍以上。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 Theranostics,2020, 10(18):8415-8429	Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800).
S2713	Geldanamycin Geldanamycin (NSC 122750) 是一种天然的HSP90抑制剂，K_d为1.2 μM，特异性干扰糖皮质激素受体(GR)/HSP联合。Geldanamycin 通过减少宿主的炎症反应来减轻病毒感染引起的ALI(急性肺损伤)/ARDS(急性呼吸窘迫综合征)。	Anal Chem,2020, 92(1):1363-1371 Anal Chem,2020, 10.1021/acs.analchem.0c02756 Cell Biol Toxicol,2020,	Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
S2639	SNX-2112 (PF-04928473) SNX-2112 (PF-04928473)选择性结合到HSP90α和HSP90β的ATP结合袋中，K_a分别为30 nM和30 nM，比17-AAG更有效。	PLoS Negl Trop Dis,2020, 17;14(4):e0008224 Onco Targets Ther,2020, 13:7907-7919 Nat Commun,2019, 10(1):402
S2656	PF-04929113 (SNX-5422) PF-04929113 (SNX-5422)是一种有效的，选择性的HSP90抑制剂，K_d为41 nM，且诱导Her-2降解，IC50为37 nM。Phase 1/2。	ACS Chem Neurosci,2019, 10(6):2890-2902 Endocrine,2016, 51(2):274-82 Antimicrob Agents Chemother,2014, 58(7):4138-44	Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.
S2685	KW-2478 KW-2478是一种非Ansamycin的HSP90抑制剂，IC50为3.8 nM。Phase 1。	Clin Exp Med,2019, 10.1007/s10238-019-00587-2
S7122	XL888 XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。Phase 1	Oncotarget,2016, 7(31):49597-49610 Clin Cancer Res,2012, 18(9):2502-14	B, XL888 (1 mmol/L, 144 hours) is effective at blocking the growth and survival of vemurafenib-resistant melanoma cell lines grown as 3D collagen-implanted spheroids. Staining shows cell viability, in which green corresponds to live cells and red: dead cells. Magnification×4.
S2930	Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ) 是一种特异性的p53抑制剂，通过降低其与Bcl-xL和Bcl-2的亲和力而发挥作用，也抑制HSP70功能和细胞自噬。	Radiat Res,2020, 193(2):119-129 Clin Transl Med,2020, 10.1002/ctm2.41 Theranostics,2019, 9(2):554-572	Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
S7282	NMS-E973 NMS-E973 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。	Immunity,2020, 52(2):328-341 Mol Cancer,2020, 19(1):112 Theranostics,2020, 10(18):8415-8429	(D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.
S8039	PU-H71 PU-H71 (NSC 750424)是有效的选择性HSP90抑制剂，IC50为51 nM。	Cancers (Basel),2020, 7;12(4) Mol Cell Biol,2020, Theranostics,2019, 9(2):554-572	Effects of low-level HSP90 inhibition (by ganetespib, 2-5 nM; PU-H71, 40-70 nM) or febrile-range temperature (39 ℃) on HSP70 and HSP90 protein levels in FANCA wild-type cells. High-level HSP90 inhibition (ganetespib, 25 nM; PU-H71, 300 nM) as well as proteotoxic proteasomal inhibition (MG132, 2.5 mM) induced the expression of HSP70. Constitutive (upper band: C) and inducible forms (lower band: I) of HSP70 are indicated. HSP90 levels are shown for comparison.
S5369	Ethoxyquin Ethoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative.
S8365	Apoptozole Apoptozole (Apoptosis Activator VII) 是热激蛋白HSP70和Hsc70的抑制剂，与HSP70和Hsc70的Kd值分别为0.14 μM和0.21 μM。它能够诱导caspase依赖性的凋亡反应。	Nat Commun,2018, 9(1):4700 Platelets,2018, 29(6):610-621	Representative images of platelets preincubated with FITC-conjugated CD41 before treated with negative control, pitstop 2, dynasore, A23, or apoptozole spreading on immobilized Fg for 10, 30, and 60 minutes, respectively. Images were taken under oil immersion with magnification × 100. Scale bar, 5 μm.
S8402	KRIBB11 KRIBB11 抑制热激诱导的荧光素酶活性，IC50为1.2 μM。它是转录因子热休克因子1(HSF1)的抑制剂。KRIBB11 可诱导生长阻滞和凋亡。	FASEB J,2020, 34(6):7927-7940 Cancer Discov,2020, CD-20-0160 Theranostics,2019, 9(10):2999-3013
S7750	KNK437 KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。	Biosci Rep,2020, 40(3) Br J Haematol,2013, 161(5):667-76 Oncol Rep,2012, 28(6):1953-8	Western blots of lysates from BaF3 JAK2 V617F cells.
S7458	VER-49009 VER-49009 (CCT0129397) 是一种强效的HSP90抑制剂，其IC50为 47 nM。
S7716	TAS-116 TAS-116是一种新型的HSP90小分子抑制剂，HSP90α和HSP90β的Ki值分别为34.7 nmol/L和21.3 nmol/L。TAS-11并不抑制其他ATP酶，如HSP70(IC50 >200 μmol/L)。
S7340	CH5138303 CH5138303 是口服有效的Hsp90抑制剂，其K_d为 0.48 nM。
S7459	VER-50589 VER-50589 是强效的HSP90抑制剂，对HSP90β的IC50为21 nM。	PLoS Negl Trop Dis,2014, 8(2):e2699
S3604	Triptolide (PG490) Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂，抑制NF-κB转录活性，破坏p65/CBP的相互作用，减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。	Cell Commun Signal,2020, 18(1):30 J Cell Physiol,2020, 4 Front Oncol,2020, 10;10:331	Spironolactone (sp.) and triptolide inhibit NER in myeloma cells. RPMI8226 cells were incubated with dimethyl sulfoxide (DMSO), spironolactone (10 μm) or triptolide (1 μm) for 6 h before NER evaluation. The figure represents the persistence of DNA-damage signal 150 min after exposure to UV (AFU: arbitrary fluorescent unit). Figure 4a shows representative merged pictures of DAPI and DDB2 proteo-probe signal (b).
S7751	VER155008 VER155008 (C07)是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。VER155008 可抑制自噬并导致HSP90客户蛋白水平降低。	Cancer Cell,2020, 37(3):371-386 Immunity,2020, 52(2):328-341 Virology,2020, 553:70-80	(D) Microglial cultures treated with 300 μM H2O2 alone or 100 μM SNAP plus 300 μM H2O2 for 24 h in the absence or presence of a chemical inhibitor (20 μM VER-155008 or 20 μM SnPP) were subjected to the determination of cell viability (MTT reduction assay). ∗p < 0.05 vs. H2O2 (300 μM) alone. +p < 0.05 vs. SNAP (100 μM) plus H2O2 (300 μM).
S6721	JG98 JG-98 是 Hsp70 的变构抑制剂，它与Hsp70家族成员保守的深袋紧密结合。JG-98 可诱导经典的凋亡特征，包括与程序性细胞死亡和膜联蛋白染色阳性相符的形态变化。JG-98 具有抗癌的活性。
S7097	HSP990 (NVP-HSP990) HSP990 (NVP-HSP990) 是一种新型有效的选择性 HSP90抑制剂，对HSP90α/β的IC50分别为0.6 nM和0.8 nM。NVP-HSP990可诱导细胞周期阻滞和凋亡。	Mol Cancer Res,2020, 10.1158/1541-7786.MCR-19-0669 Theranostics,2020, 10(18):8415-8429 Mol Pharm,2019, 16(5):2069-2082	Expression of CD24 and CD44 in HSP90 inhibitor‐treated, shRNA‐transduced HCC1937 cells was analyzed by flow cytometry.

目录号	产品描述	文献引用	实验数据
S0279^New	Dimethylenastron Dimethylenastron 是一种有效的、特异性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制剂，其IC50值为200 nM。Dimethylenastron 可诱导人多发性骨髓瘤细胞的有丝分裂停滞和凋亡并上调 Hsp70 的表达。
S0294^New	HSF1A HSF1A 是一种可透过细胞的 heat shock transcription factor 1 (HSF1) 的激活剂。HSF1A 可保护细胞免受压力诱导的凋亡，结合TRiC亚基并抑制TRiC活性，而不会干扰ATP水解。
S1972	Tamoxifen Citrate Tamoxifen Citrate (ICI 46474) 是一种雌激素受体 estrogen receptor 调节剂 (SERM)，通过竞争性抑制雌激素结合发挥作用。Tamoxifen Citrate 也是一种有效的 Hsp90 激活剂，可增强Hsp90分子伴侣ATPase的活性。Tamoxifen 可诱导凋亡与自噬。	Acta Biomater, 2020, S1742-7061(20)30695-4 Molecules, 2020, 25(15)E3355 Molecules, 2020, 25(20)E4606	Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells.
S6568	ML346 ML346是Hsp70激活剂，是一种新型的蛋白质稳定状态调节剂。
S1238	Tamoxifen Tamoxifen (ICI 46474) 作用于乳腺组织，是一种雌激素受体estrogen receptor调节剂 (SERM)。Tamoxifen可增强Hsp90分子伴侣ATPase的活性。Tamoxifen可诱导凋亡。	Cell, 2020, S0092-8674(20)31394-5 Aging Dis, 2020, 9;11(3):523-535 Bone, 2020, 130:115123	E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01.

目录号	产品描述	文献引用	实验数据
S1052	Elesclomol (STA-4783) Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。Phase 3。	Nat Commun, 2020, 15;11(1):2423 EBioMedicine, 2020, 54:102715 Cancers (Basel), 2020, 12(6):E1645
S8305	TRC051384 TRC051384是heat shock protein 70 (HSP70)的诱导物，同时也是有效的抗炎药。
S8299	HA15 HA15是特异靶向BiP/GRP78/HSPA5的小分子。在所检测的黑色素瘤细胞中具有抗肿瘤活性，包括从病人中分离得到的细胞和对BRAF抑制剂具有耐药性的细胞。	Am J Cancer Res, 2020, 10(8):2621-2634 J Pharm Biomed Anal, 2020, 185:113230 Cell Death Dis, 2019, 10(9):651	SP cells in inhibitor-treated, shRNA-transduced HCC1937 cells analyzed by flow cytometry using Hoechst 33342 dye. Data are shown as mean±SD. **P<.0001, P<.001, P<.01, P<.05.

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S1052