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使用 'EZH2' 作为标签的产品

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CPI-169

Catalog No. A15920
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EZH2 抑制剂

CPI-169是一种有效的选择性EZH2抑制剂，对EZH2 WT，EZH2 Y641N和EZH1的IC50分别为0.24 nM，0.51 nM和6.1 nM。了解更多

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EPZ-6438 (Tazemetostat)

Catalog No. A12712
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EZH2 抑制剂

EPZ-6438 (Tazemetostat)是一种有效的，选择性的，口服可利用的EZH2酶促活性小分子抑制剂，无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM。它诱导SMARCB1缺失的MRT细胞中的凋亡和分化。了解更多

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- Wang Z, .et al. Targeting EZH 2 as a novel therapeutic strategy for sorafenib‐resistant thyroid carcinoma, J Cell Mol Med, 2019, May 13 PMID: 31087496
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609
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EPZ005687

Catalog No. A12439
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EZH2 抑制剂

EPZ005687是EZH2的有效抑制剂 (Ki为24 nM)。了解更多

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GSK126

Catalog No. A11757
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EZH2 抑制剂

GSK126是一种有效的，高选择性的，具有S-腺苷甲硫氨酸竞争性的小分子EZH2甲基转移酶活性抑制剂，可降低总体H3K27me3水平并重新激活沉默的PRC2目标基因。了解更多

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- Lucy E. Dawson, .et al. Induction of Myogenic Differentiation Improves Chemosensitivity of Chemoresistant Cells in Soft-Tissue Sarcoma Cell Lines, Sarcoma, 2020, 2020: 8647981 PMID: 32300280
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Dupret B, .et al. The histone lysine methyltransferase Ezh2 is required for maintenance of the intestine integrity and for caudal fin regeneration in zebrafish, Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 PMID: 28887218
- Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609
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GSK343

Catalog No. A13114
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EZH2 抑制剂

GSK343是有效的组蛋白H3-赖氨酸27（H3K27）甲基转移酶EZH2抑制剂（IC = 4 nM）。对除EZH1以外的其他HMT的选择性是1000倍（选择性是60倍）。GSK343抑制HCC1806细胞中的H3K27甲基化，IC小于200nM（通过免疫荧光测量）。了解更多

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- Nie L, .et al. CDK2-mediated site-specific phosphorylation of EZH2 drives and maintains triple-negative breast cancer, Nat Commun, 2019, Nov 8;10(1):5114 PMID: 31704972
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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GSK503

Catalog No. A15549
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EZH2 抑制剂

GSK-503是一种有效的EZH2抑制剂，具有潜在的抗癌活性。了解更多

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UNC-1999

Catalog No. A13166
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EZH2/EZH1 抑制剂

UNC-1999是生物可利用抑制剂，对野生型和突变型ezh2以及ezh1具有高体外效力，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。了解更多

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- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48

Adooq Bioscience

使用 'EZH2' 作为标签的产品

CPI-169

EPZ-6438 (Tazemetostat)

EPZ005687

GSK126

GSK343

GSK503

UNC-1999

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