Autophagy

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S8764	IITZ-01	<1 mg/mL	100 mg/mL	<1 mg/mL
S9424	Liensinine diperchlorate		50 mg/mL
S9150	Daurisoline		64 mg/mL
S3758	Sinomenine hydrochloride	-1 mg/mL	73 mg/mL	-1 mg/mL
S1105	LY294002	<1 mg/mL	36 mg/mL	21 mg/mL
S1150	Paclitaxel	<1 mg/mL	171 mg/mL	18 mg/mL
S2758	Wortmannin	<1 mg/mL	85 mg/mL	<1 mg/mL
S2767	3-Methyladenine (3-MA)	10 mg/mL	3 mg/mL	4 mg/mL
S2775	Nocodazole	<1 mg/mL	7 mg/mL	<1 mg/mL
S4157	Chloroquine Phosphate	100 mg/mL	<1 mg/mL	<1 mg/mL
S1835	Azithromycin	<1 mg/mL	100 mg/mL	100 mg/mL
S7289	PFK15	<1 mg/mL	19 mg/mL	2 mg/mL
S7885	SBI-0206965	<1 mg/mL	97 mg/mL	10 mg/mL
S8576	EAD1	100 mg/mL	100 mg/mL	100 mg/mL
S7888	Spautin-1	<1 mg/mL	54 mg/mL	7 mg/mL
S8317	3BDO	<1 mg/mL	65 mg/mL	49 mg/mL
S7811	MHY1485	<1 mg/mL	4 mg/mL	<1 mg/mL
S8596	Autophinib	<1 mg/mL	69 mg/mL	<1 mg/mL
S8369	Lys05	3 mg/mL	9 mg/mL	<1 mg/mL
S4430	Hydroxychloroquine Sulfate	67 mg/mL	<1 mg/mL	<1 mg/mL
S7949	MRT68921 HCl	<1 mg/mL	<1 mg/mL	<1 mg/mL
S7683	PIK-III	<1 mg/mL	63 mg/mL	63 mg/mL
S8527	ROC-325	<1 mg/mL	4 mg/mL	4 mg/mL
S1047	Vorinostat (SAHA, MK0683)	<1 mg/mL	52 mg/mL	3 mg/mL
S1002	ABT-737	<1 mg/mL	100 mg/mL	<1 mg/mL
S1049	Y-27632 2HCl	14 mg/mL	64 mg/mL	<1 mg/mL
S1039	Rapamycin (Sirolimus)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1023	Erlotinib HCl (OSI-744)	<1 mg/mL	4 mg/mL	<1 mg/mL
S9027	Corynoxine	<1 mg/mL	77 mg/mL	77 mg/mL
S9310	Isorhychophylline		77 mg/mL
S5312	Urolithin A	<1 mg/mL	45 mg/mL	<1 mg/mL
S8595	Tat-beclin 1 (Tat-BECN1)	100 mg/mL	-1 mg/mL	-1 mg/mL
S1057	Obatoclax Mesylate (GX15-070)	<1 mg/mL	83 mg/mL	<1 mg/mL
S1038	PI-103	<1 mg/mL	24 mg/mL	<1 mg/mL
S1149	Gemcitabine HCl	19 mg/mL	<1 mg/mL	<1 mg/mL
S2218	Torkinib (PP242)	<1 mg/mL	61 mg/mL	18 mg/mL
S1237	Temozolomide	<1 mg/mL	38 mg/mL	<1 mg/mL
S1950	Metformin HCl	33 mg/mL	<1 mg/mL	<1 mg/mL
S1573	Fasudil (HA-1077) HCl	65 mg/mL	5 mg/mL	<1 mg/mL
S1972	Tamoxifen Citrate	<1 mg/mL	100 mg/mL	100 mg/mL
S2827	Torin 1	<1 mg/mL	2 mg/mL	<1 mg/mL
S1396	Resveratrol	<1 mg/mL	45 mg/mL	<1 mg/mL
S1322	Dexamethasone (DHAP)	<1 mg/mL	79 mg/mL	6 mg/mL
S1714	Gemcitabine	52 mg/mL	52 mg/mL	<1 mg/mL
S7046	Brefeldin A	<1 mg/mL	4 mg/mL	<1 mg/mL
S2713	Geldanamycin	<1 mg/mL	36 mg/mL	<1 mg/mL
S2929	Pifithrin-α (PFTα) HBr	<1 mg/mL	67 mg/mL	<1 mg/mL
S3030	Niclosamide	<1 mg/mL	<1 mg/mL	<1 mg/mL
S1389	Omeprazole	<1 mg/mL	69 mg/mL	13 mg/mL
S1979	Amiodarone HCl	<1 mg/mL	23 mg/mL	11 mg/mL
S2480	Loperamide HCl	<1 mg/mL	22 mg/mL	4 mg/mL
S4028	Dexamethasone Sodium Phosphate	103 mg/mL	<1 mg/mL	<1 mg/mL
S1693	Carbamazepine	<1 mg/mL	47 mg/mL	18 mg/mL
S2458	Clonidine HCl	53 mg/mL	53 mg/mL	53 mg/mL
S1837	Flubendazole	<1 mg/mL	3 mg/mL	<1 mg/mL
S1747	Nimodipine	<1 mg/mL	84 mg/mL	84 mg/mL
S3124	Dexamethasone Acetate	<1 mg/mL	87 mg/mL	20 mg/mL
S2491	Nitrendipine	<1 mg/mL	72 mg/mL	<1 mg/mL
S3653	Spermidine trihydrochloride	50 mg/mL	30 mg/mL	<1 mg/mL
S4081	Sulfacetamide Sodium	51 mg/mL	19 mg/mL	<1 mg/mL
S8240	SMER28	<1 mg/mL	52 mg/mL	52 mg/mL
S1238	Tamoxifen	<1 mg/mL	74 mg/mL	74 mg/mL
S1241	Vincristine sulfate	60 mg/mL	100 mg/mL	<1 mg/mL
S1168	Valproic acid sodium salt (Sodium valproate)	33 mg/mL	33 mg/mL	33 mg/mL
S1041	STF-62247	<1 mg/mL	53 mg/mL	3 mg/mL
S4750	Sulfacetamide sodium salt hydrate	50 mg/mL	50 mg/mL	2 mg/mL

Autophagy抑制剂（66）
新Autophagy产品

产品目录	产品描述	文献引用	实验数据
S8764^New	IITZ-01 IITZ-01是一种有效的自噬（autophagy）抑制剂，可增强自噬体的积累，但通过破坏溶酶体功能抑制自噬体的退化。
S9424^New	Liensinine diperchlorate Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.
S9150^New	Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
S3758^New	Sinomenine hydrochloride Sinomenine (SN), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
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。	Nature, 2015, 10.1038/nature14412 Am J Respir Crit Care Med, 2015, 10.1164/rccm.201501-0188OC Blood, 2014, 123(2):239-48	Type I IFNs induce ISG expression in a serine phosphorylation-independent manner. Cells were treated with kinase inhibitors (SB203580, rottlerin, Ly294002, PD98059, and SP600125) before stimulation with IFN-a and IFN-b for 6 hours. Cell lysates were used in western blotting and probed for serine phosphorylation.The relative amounts of pSTAT1 S727 in (up-graph) were quantied and normalized to an untreated control (below-graph).
S1150	Paclitaxel Paclitaxel是一种microtubule聚合物稳定剂，在人内皮细胞中IC50为0.1 pM。	Nature, 2017, 551(7679):247-250 Science, 2017, eaal3755 Sci Transl Med, 2018, 10(433)	(F) Kaplan-Meier curves are shown for all groups described: no hydrogel, a hydrogel loaded with paclitaxel, or a hydrogel loaded with doxorubicin. The number of mice per group (n) and median survival (ms) are listed. The experiment was performed at least three times.
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。	Nature, 2015, 10.1038/nature14412 Science, 2016, 353(6302):929-32 Cancer Res, 2014, 74(10):2846-56	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.
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）。	Redox Biol, 2018, 18:138-157 Cancer Lett, 2018, 416:24-30 Cell Death Dis, 2016, 7(6):e2247	MDC-labeled vacuoles were induced by AZD2014 and inhibited by autophagy inhibitor (3-MA). SMMC-7721 cells were treated with AZD2014 or rapamycin at concentrations of 100 and 600 nM, respectively, for 48 hours in the presence or absence of 3-MA, and then stained with MDC. Cells were immediately observed under a confocal microscope. Cells in the control group were treated with DMSO. bars, 20 μm.
S2775	Nocodazole Nocodazole是一种微管聚合的快速可逆抑制剂，也抑制Abl， Abl(E255K)和Abl(T315I)，IC50分别为0.21 μM， 0.53 μM和0.64 μM。Nocodazole可提高CRISPR介导的同源重组效率，对增强精确的基因编辑效力具有加成作用。	J Immunol, 2015, 10.4049/jimmunol.1402897 J Biol Chem, 2016, 10.1074/jbc.M116.722751 Cell Signal, 2016, 28(12):1826-1832	A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively.
S4157	Chloroquine Phosphate Chloroquine Phosphate是一种4-氨基喹啉的抗疟疾和抗风湿药，也是一种ATM激活剂。	Leukemia, 2017, 10.1038/leu.2016.325 Cell Signal, 2016, 28(8):1086-98 Int J Mol Med, 2017, 10.3892/ijmm.2017.3008	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.
S1835	Azithromycin Azithromycin是一种抑制蛋白合成的抗生素，用于细菌感染的治疗。
S7289	PFK15 PFK15 是一种强效的选择性的6-phosphofructo-2-kinase (PFKFB3)抑制剂，其IC50为207 nM。	Br J Pharmacol, 2017, 174(9):893-908 J Exp Clin Cancer Res, 2017, 10.1186/s13046-016-0481-1 PLoS One, 2016, 11(9):e0163768	RA FLSs were pretreated with DMSO (as the control) or various concentrations of a specific PFKFB3 inhibitor, PFK15, for 4 h (A). The expression of IL-6, IL-8, CCL-2 and CXCL-10 was measured by real-time qPCR. The data are representative of independent experiments (means ± SEM) from10 RA patients. *P < 0.05, significantly different from control or SiC; #P < 0.05, significantly different from treatment with TNF-α alone
S7885	SBI-0206965 SBI-0206965是一种高度选择性自吞噬激酶ULK1抑制剂，IC50为108 nM，选择性比作用于ULK2高7倍。	Biochim Biophys Acta, 2017, 1863(11):2796-2807	Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, p < 0.01, * p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05.
S8576	EAD1 EAD1是一种有效的自噬（autophagy）抑制剂，在BxPC3细胞中IC50为5.8 μM。它在肺癌和胰腺癌细胞中具有抗增殖活性。
S7888	Spautin-1 Spautin-1是一种有效的特异性autophagy抑制剂，抑制USP10 和 USP13的去泛素化活性，IC50为∼0.6-0.7 μM。	Int J Cancer, 2015, 136(11):2717-29 J Hematol Oncol, 2016, 9(1):45 Cancer Lett, 2018, 425:1-12	Autophagosomal inhibition was performed in 32D EV, WT CALR, del52, and ins5 expressing cells. The 32D cell lines were treated with the inhibitor spautin-1 for the indicated time. Lysates were prepared, and SDS-PAGE and Western blotting were performed. Antibodies detecting mutated CALR (CALR mut), CALR, LC3I-II, and GAPDH were used for immunostaining. LC3I-II served as control for successful autophagosomal inhibition.
S8317	3BDO 3BDO是一种丁内酯衍生物，可靶向FKBP1A并激活mTOR信号通路，抑制HUVECs自噬。
S7811	MHY1485 MHY1485是一种有效的，细胞渗透性 mTOR 激动剂，也能有效抑制 autophagy。	Biochem J, 2017, 474(16):2733-2747 Mol Med Rep, 2016, 14(4):3662-8	MYH1485, an activator of mTOR, reduced LC3II production and inhibited autophagosome formation in PAR2-knockdown cells.
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。
S8369	Lys05 Lys05是一种新型的溶酶体自噬抑制剂，可有效地在细胞和肿瘤中的溶酶体中积累并降低溶酶体的酸度，从而导致发挥对自噬和肿瘤生长的持续抑制作用。
S4430	Hydroxychloroquine Sulfate Hydroxychloroquine Sulfate是一种抗疟疾药，用于治疗系统性红斑狼疮，类风湿关节炎等自身免疫病，炎症以及皮肤病。它也是autophagy和toll-like receptor (TLR) 7/9的抑制剂。	Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1489 Cell Death Dis, 2017, 8(1):e2558 Oxid Med Cell Longev, 2017, 8519169	C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
S7949	MRT68921 HCl MRT68921是一个高效的双重的自噬激酶ULK1/2抑制剂，其IC50分别为2.9 nM和1.1 nM。	Methods Enzymol, 2017, 587:391-404
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。	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
S8527	ROC-325 ROC-325是具有口服活性的溶酶体介导的自噬抑制剂，可减少AML细胞的细胞活性，IC50范围为0.7-2.2 μM。
S1047	Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA)是一种HDAC抑制剂，无细胞试验中IC50为~10 nM。	Nature, 2011, 471(7337):235-9 Nature, 2017, 551(7679):247-250 Nat Biotechnol, 2011, 29(3):255-65	Activity of vorinostat in Jurkat and Peer T-ALL cell lines in an MTT cell viability assay. Cells were treated with increasing drug concentrations for 72 h. The data are plotted as the mean % of DMSO-treated control cells against the corresponding drug concentration. The error bars are the standard error. For each drug and cell line, 3-4 independent experiments were performed with 6 replicates at each drug concentration.
S1002	ABT-737 ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-w，无细胞试验中EC50分别为78.7 nM，30.3 nM和197.8 nM；但对Mcl-1， Bcl-B及Bfl-1没有抑制作用。Phase 2。	Nature, 2017, 551(7679):247-250 Nat Biotechnol, 2011, 29(6):542-6 Nat Med, 2013, 19(11):1478-88	Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
S1049	Y-27632 2HCl Y-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂，无细胞试验中K_i为140 nM，比对其他激酶包括PKC，cAMP依赖性蛋白激酶，MLCK和PAK的作用强200多倍。	Nature, 2018, 557(7704):256-260 Nature, 2016, 532(7597):107-11 Cell, 2018, 174(2):338-349	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1039	Rapamycin (Sirolimus) Rapamycin (Sirolimus)是一种特定的 mTOR 抑制剂，在 HEK293细胞中，IC50 为 ~0.1 nM。	Nature, 2016, 539(7629):437-442 Nature, 2016, 532(7599):389-93 Nat Genet, 2014, 46(4):364-70	Protein blots showing MYC expression in naive and persister cells after 3 d of treatment with 2 uM AKT inhibitor MK-2206 (AKTi) or 10 nM mTOR inhibitor rapamycin (Rapa).
S1023	Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744)是一种EGFR抑制剂，在无细胞试验中IC50为2 nM，对EGFR的选择性比对人c-Src或v-Abl高1000多倍。	Cell, 2012, 151(5):937-50 Nat Genet, 2012, 44(8):852-60 Cancer Discov, 2013, 3(12):1404-15	Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers.
S9027^New	Corynoxine Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.
S9310^New	Isorhychophylline Isorhynchophylline is a major tetracyclic oxindole alkaloid isolated from the Chinese herbal medicine Uncaria rhynchophylla (Miq.)Jacks (Gouteng in Chinese). It acts as a neuronal autophagy inducer with therapeutic potential for cardiovascular and central nervous system diseases.
S5312^New	Urolithin A Urolithin A, a metabolite of ellagitannin, is a first-in-class natural compound that induces mitophagy both in vitro and in vivo following oral consumption.
S8595^New	Tat-beclin 1 (Tat-BECN1) Tat-beclin 1 (Tat-BECN1)能够通过动员内源性Beclin 1刺激自噬，改善临床疗效。
S1057	Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂，无细胞试验中K_i为0.22 μM，可以协助抑制MCL-1介导的抗细胞凋亡作用。Phase 3。	Nat Chem Biol, 2015, 10.1038/nchembio.1986 Cancer Res, 2011, 71(13):4494-505 Cancer Res, 2012, 72(12):3069-79	In vivo antitumor efﬁcacies of AZD2281 and GX15-070 alone or in combination in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 lm-thick slides for H&E, PCNA, and CD34 staining.
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。	Cell, 2013, 153(4):840-54 Leukemia, 2013, 27(3):650-60 Leukemia, 2012, 26(5):927-33	(D) IGROV parental, shControl (two independent clones) and ShPKCiota (two independent clones) were treated with 5 μM GDC-0941 and 1.5 μM PI-103 for 24 hours and subjected to western blot analysis with the indicated antibodies. Each experiment was performed in triplicate.
S1149	Gemcitabine HCl Gemcitabine HCl是一种DNA synthesis抑制剂，作用于PANC1，MIAPaCa2，BxPC3和Capan2细胞，IC50分别为50 nM， 40 nM， 18 nM和12 nM。	Sci Transl Med, 2015, 7(284):284ra57 Nucleic Acids Res, 2014, 42(10):6436-47 Clin Cancer Res, 2014, 20(12):3187-97	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
S2218	Torkinib (PP242) Torkinib (PP242)是一种选择性的mTOR抑制剂，在无细胞试验中IC50为8 nM；靶向作用于mTOR复合体，作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。	Science, 2016, 353(6302):929-32 Nat Chem Biol, 2013, 9(11):708-14 J Clin Invest, 2015, 10.1172/JCI78018	MTORC1 regulates the subcellular distribution of TFEB. Immunofluorescence confocal microscopy showing nuclear localization of recombinant TFEB-Flag in ARPE-19 cells incubated with MTORC1 inhibitors (PP242, LY294002, Wortmannin).
S1237	Temozolomide Temozolomide(TMZ)是一种单功能的SN-1烷化剂，修饰DNA环上的氮原子以及环外氧基团。在生理pH值下，TMZ转化为活性产物MTIC、降解为methyldiazonium cation，后者再将甲基转移到DNA, 阻碍DNA复制启动，诱使细胞凋亡，是一种DNA损伤诱导剂。	Nat Med, 2015, 10.1038/nm.3855 Clin Cancer Res, 2014, 20(6):1555-65 Clin Cancer Res, 2017, 23(2):523-535	C57BL/6 mice were implanted in the striatum with citrine-GL26-Cherry-HMGB1, which were stably transfected to express the YFP citrine and HMGB1 fused to red fluorescent protein cherry. Fourteen days later, they were treated with saline, Ad-TK+Ad-Flt3L, or Ad-TK+Ad-Flt3L+TMZ (temozolomide). Five days after treatment, the cellular location of cherry-HMGB1 in these cells was assessed by confocal microscopy. Arrows, tumor cells (green) with cytoplasmic HMGB1 (red).
S1950	Metformin HCl Metformin HCl 降低肝细胞中高血糖症，主要通过抑制肝糖原的产生（肝脏糖异生作用)发挥作用。	Cancer Cell, 2014, 26(6):840-50 Luminescence, 2014, 29(1):65-73 Sci Rep, 2017, 7(1):2169	Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。	J Clin Invest, 2014, 124(9):3757-66 J Clin Invest, 2014, 124(4):1646-59 Biosens Bioelectron, 2016, 86:508-515	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1972	Tamoxifen Citrate Tamoxifen Citrate是一种雌激素受体拮抗剂，通过竞争性抑制雌激素结合发挥作用。	University of North Texas, 2014, Timothy E. Richardson	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.
S2827	Torin 1 Torin 1是一种有效的mTORC1/2抑制剂，在无细胞试验中IC50为2 nM/10 nM；作用于mTOR比作用于PI3K选择性高1000倍。	Cancer Discov, 2016, 6(7):727-39 Elife, 2015, 4 Am J Pathol, 2014, 184(1):214-29	Huh-7.5 cells were treated with increasing concentration of Torin 1, a known autophagy inducer, and the autophagy response was assessed by measuring LC3II and p62 levels.
S1396	Resveratrol Resveratrol具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。	Cell Physiol Biochem, 2015, 35(6):2255-2271 Biochim Biophys Acta, 2016, 1859(2):294-305 Molecules, 2014, 19(12):20570-9	PC-9 and A549 cells were treated with 100 nM siRNA against PUMA and 100 nM negative control (NC) siRNA for 12 h, and treated with the indicated concentrations of RV and ERL in combination for an additional 48 h. The knockdown effects on PUMA were confirmed by Western blot analysis.
S1322	Dexamethasone (DHAP) Dexamethasone (DHAP)是一种有效的半合成的糖皮质激素类甾体药物，也是一种interleukin receptor调节剂，具有抗炎和免疫抑制作用。	Clin Cancer Res, 2018, 24(4):927-938 Leukemia, 2017, 31(12):2652-2660 Oncogene, 2017, 36(40):5631-5638	Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
S1714	Gemcitabine Gemcitabine是核酸合成抑制剂，是有效、特异的脱氧胞苷类似物，用于化疗。	Nature, 2017, 552(7683):116-120 Cancer Discov, 2011, 1(4):352-65 Sci Transl Med, 2015, 7(284):284ra57	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
S7046	Brefeldin A Brefeldin A 作用于HCT 116细胞，抑制内酯抗生素和ATPase，作用于protein transport（蛋白转运），IC50为0.2 μM，诱导癌细胞分化和凋亡。它还能提高同源重组修复效率，是CRISPR-mediated HDR的增强剂。	Nanoscale, 2018, 10(18):8796-8805 EBioMedicine, 2017, 18:188-198 EBioMedicine, 2018, 36:229-240	Immunofluorescence staining of LC3 protein expression of U2OS cells treated with DMSO (negative control), Rap (positive control, 500 nM), Tha (1 μM), Tun (2 μg/mL), BFA (10 μg/mL), and DTT (4 mM) for 8 h. Immunoblot of ER-phagy-related proteins of U2OS cells treated with four ER stress inducers.
S2713	Geldanamycin Geldanamycin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。	J Antimicrob Chemother, 2015, 10.1093/jac/dku549 Antimicrob Agents Chemother, 2015, 59(8):4727-33 PLoS One, 2015, 10(9):e0138936	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.
S2929	Pifithrin-α (PFTα) HBr Pifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。	Nanoscale, 2017, 9(20):6765-6776 Am J Transplant, 2015, 15(12):3095-111 Acta Biomater, 2017, 49:541-554	(C) Cell viability was measured after TSA and PFTα co-treatment. MG63 were exposed to TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment compared with TSA treatment alone for 24h. Data are presented as means ± S.E.M. from 3 independent experiments. , P < 0.05 vs. MG63 cells without TSA or PFTα treatment; *, P < 0.01 vs. MG 63 cells without TSA or PFTα treatment; &&, P < 0.01 vs. MG63 cells with TSA treatment alone. (D) Flow cytometry analysis of ANXA5 and propidiumiodide staining of MG63 cells with TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment, compared with TSA treatment alone.
S3030	Niclosamide Niclosamide能够抑制DNA复制，并抑制STAT3，无细胞试验中IC50为0.7 μM。 Niclosamide 选择性地抑制STAT3的磷酸化，对其他同系物如STAT1和STAT5的激活没有明显抑制作用。	Int Immunopharmacol, 2016, 36:199-204 Onco Targets Ther, 2017, 10:1767-1776	Bacterial infection in IPEC-J2 cells. The invasion and attachment of EHECO157:H7 was increased in the IPEC-J2 cells in the presence of 1 μM niclosamide. Data are expressed as the mean ± SEM (n= 6). Differences between groups were determined by paired samples t-test. *P<0.05 compared with the control.
S1389	Omeprazole Omeprazole 是一种质子泵抑制剂，用于治疗消化不良，消化性溃疡，胃食管逆流，咽喉逆流。
S1979	Amiodarone HCl Amiodarone HCl是一种sodium/potassium-ATPase抑制剂同时也是自噬的激活剂，用于治疗各种心律失常。	Toxicol Appl Pharmacol, 2015, 285(1):51-60	Drugs across therapeutic indications induce lipid formation in hiPS-CM. Lipid accumulation was detected in cardiac cells using the LipidTox plate-based fluorescent assay on the Thermo Scientific CellInsight High Content platform. A) Ten drugs increased lipid levels in hiPS-CM following 48 h treatment. The lowest drug dose that induced a N1.5-fold increase in lipid formation is shown. B) Representative images (20×) from the assay are shown to the right. All drugs had >55% cell viability at 48 h at these tested concentrations. C) Of these 10 drugs, 8 significantly increased lipid accumulation following only 24 h treatment (images not shown). All drugs had >80% cell viability at 24 h at these drug doses. The graphs represent the mean fold-change of the lowest concentration of drug that significantly induced lipid formation >1.5-fold more than vehicle control. P<0.05, P<0.01, and **P<0.0001.
S2480	Loperamide HCl Loperamide HCl是一种阿片受体激动剂，ED50为0.15 mg/kg。	Antimicrob Agents Chemother, 2014, 58(8):4875-84 Neurogastroenterol Motil, 2016, 28(8):1241-51	Low-micromolar amounts of loperamide inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 8 μM LPM (C). Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
S4028	Dexamethasone Sodium Phosphate Dexamethasone Sodium Phosphate是一种白介素受体抑制剂，抑制COX-2。		Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
S1693	Carbamazepine Carbamazepine 是一种钠离子通道抑制剂，作用于大鼠脑突触体时， IC50为131 μM。
S2458	Clonidine HCl Clonidine HCl 是一种直接起作用的α2肾上腺素能受体激动剂，ED50为0.02±0.01 mg/kg。
S1837	Flubendazole Flubendazole 是一种驱虫剂，作用于MDAY-D2 细胞，IC50为3 nM。		Inhibitory curves and IC50 values for the reference compound flubendazole (B) against VEGFR2.
S1747	Nimodipine Nimodipine是一种二氢吡啶衍生物，是钙离子通道抑制剂Nifedipine的类似物，具有降压活性。Nimodipine能减少细胞内游离Ca2+，Beclin-1及细胞自噬。	Antiviral Res, 2016, 132:38-45 Antiviral Res, 2016, 132:38-45	Assessment of the role of Ca2+ channels during RSV replication. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with calcium channel blockers nifedipine, nimodipine, and tetrandrine (A), at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. NS, no differences at a significance level of 0.05.
S3124	Dexamethasone Acetate Dexamethasone 是一种有效的糖皮质激素类合成物，属于类固醇药物。Dexamethasone用于很多炎症和自身免疫病的治疗，例如风湿性关节炎和支气管痉挛。接受化疗的癌症病人服用dexamethasone去抵消部分化疗带来的副作用。Dexamethasone 也用在诊断方面，利用它能抑制垂体一肾上腺轴特性。		Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
S2491	Nitrendipine Nitrendipine是一种二氢吡啶类钙离子通道抑制剂，IC50为95 nM。
S3653	Spermidine trihydrochloride Spermidine是一种从腐胺和dcSAM中，通过亚精胺合成酶合成的天然聚胺。它是新型的自噬诱导剂，负向调控N-methyl-d-aspartate (NMDA)。
S4081	Sulfacetamide Sodium Sulfacetamide Sodium是一种抗生素。
S8240	SMER28 SMER28是一种细胞自噬的增强剂，可独立于雷帕霉素、在哺乳动物细胞中诱导细胞自噬。
S1238	Tamoxifen Tamoxifen作用于乳腺组织，是一种雌激素受体拮抗剂。	Oncogene, 2017, 36(16):2255-2264 Environ Pollut, 2018, 234:846-854 University of North Texas, 2014, Timothy E. Richardson	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.
S1241	Vincristine sulfate Vincristine sulfate通过与微管蛋白结合而抑制微管聚合，IC50为32 μM。	Cancer Res, 2013, 73(20):6310-22 J Pharmacol Exp Ther, 2014, 350(3):646-56 Int J Mol Sci, 2012, 13(9):10736-49	Plk inhibitor cooperates with chemotherapeutic agents. Conditional patched mutant tumor cells were treated with increasing concentrations of the chemotherapeutic agents vincristine alone or in combination with 10 nMol/L BI-2536. Cells were cultured for 48 hours, pulsed with 3H-Td, and harvested for analysis of 3H-Td incorporation at 66 hours.
S1168	Valproic acid sodium salt (Sodium valproate) Valproic acid sodium salt (Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Neurosci, 2013, 33(17):7535-47 Cell Death Dis, 2016, 7:e2221	(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
S1041	STF-62247 STF-62247是一种靶向具有VHL缺陷的肾细胞癌的小分子化合物，诱导自噬。STF-62247对缺乏VHL的肾细胞具有选择毒性和抑制细胞生长作用;作用于VHL缺陷的细胞比作用于野生型(VHL+)选择性高25倍。	Neuropsychiatr Dis Treat, 2015, 11:2091-9	Columns depict relative densitometric values that were obtained by comparing with (β-actin. Presenilin 1, Nicastrin, and Pen-2 were increased with the 3-MA treatment (P<0.001) while the other component of the γ-secretase complex (APH-1 and Presenilin 2) has no difference, compared with the STF-62247 treatment. Moreover, Bace1 and ADAM17 respectively had no difference between 3-MA and STF-62247 treatments. Both autophagy inhibitor and inducer activated α-, β-, and γ-secretases (P<0.005). Abbreviations: Aβ, beta-amyloid; ADAM17, a disintegrin and metalloprotease 17; APH-1, anterior pharynx-defective 1; APP, amyloid protein precursor; Bace1, beta-site APP cleavage enzyme; 3-MA, 3-methyladenine; Con, control, LC3, microtubule-associated protein 1A/1B-light chain 3.
S4750	Sulfacetamide sodium salt hydrate Sulfacetamide是一种磺胺类抗生素，通过抑制dihydropteroate synthase(DHPS)阻滞二氢叶酸的合成。Sulfacetamide是细菌para-aminobenzoic acid (PABA)的竞争性抑制剂，PABA是细菌合成叶酸所必需的。

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