GSK126 (GSK2816126A) | EZH2抑制剂 - MCE
GSK126 (GSK2816126A) 是一种有效，选择性的 EZH2 甲基转移酶抑制剂， IC50 为 9.9 nM。 * Please select Quantity before adding items. • Cell. 2018 Sep 20;175 (1):186-199.e19. [Abstract] • Blood. 2022 Aug 19;blood.2022015668. [Abstract] • J Exp Med. 2018 May 7;215 (5):1365-1382. [Abstract] • Carbohydr Polym. 2024 Dec 15:346:122645. [Abstract]
GSK-2816126(GSK-2816126) - 药物靶点：EZH2_在研适应症：去 …
最初是开发用于治疗ezh2激活突变的淋巴瘤，临床前研究中gsk2816126对ezh2表现出高选择性（超过ezh1的100倍），此外，gsk2816126在纳摩尔浓度下诱导体外癌细胞死亡，并在ezh2突变体dlbcl的异种移植模型中显示出显著的抗肿瘤活性。
Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2
2019年12月15日 · Purpose: Enhancer of zeste homolog 2 (EZH2) activity is dysregulated in many cancers. Patients and methods: This phase I study determined the safety, maximum-tolerated dose (MTD), pharmacokinetics, and pharmacodynamics of the intravenously administered, highly selective EZH2 inhibitor, GSK2816126, (NCT02082977).
GSK126 | 99.84%(HPLC) | Histone Methyltransferase inhibitor
2024年5月22日 · GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. In vitro, GSK126 most potently inhibits H3K27me3, followed by H3K27me2 in both EZH2 wild-type and mutant DLBCL cell lines.
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A phase I, open-label study of GSK2816126, an enhancer of zeste …
2016年5月20日 · GSK2816126, a selective and potent inhibitor of wild-type (WT) and mutant EZH2, can decrease H3K27me3 levels in vitro and has demonstrated antiproliferative activity in several cell lines derived from EZH2 WT/mutant cancers.
A Phase I Study of GSK2816126, an Enhancer of Zeste Homolog …
GSK2816126, a highly selective and potent inhibitor of both wild type (wt) and mutant (mut) EZH2, decreases H3K27 tri-methylation, releases transcriptional repression of PRC2 target genes and induces anti-proliferative activity in several EZH2 wt/mut cancer cell lines.
A Phase I Study of GSK2816126, an Enhancer of Zeste
GSK2816126, a highly selective and potent inhibitor of both wild type (wt) and mutant (mut) EZH2, decreases H3K27 tri-methylation, releases transcriptional repression of PRC2 target genes and induces anti-proliferative activity in several EZH2 wt/mut cancer cell lines.
Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) …
2019年12月13日 · This phase I study determined the safety, maximum-tolerated dose (MTD), pharmacokinetics, and pharmacodynamics of the intravenously administered, highly selective EZH2 inhibitor, GSK2816126, (NCT02082977). Doses of GSK2816126 ranged from 50 to 3,000 mg twice weekly, and GSK2816126 was given 3-weeks-on/1-week-off in 28-day cycles.
Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) …
PURPOSE: Enhancer of zeste homolog 2 (EZH2) activity is dysregulated in many cancers. PATIENTS AND METHODS: This phase I study determined the safety, maximum-tolerated dose (MTD), pharmacokinetics, and pharmacodynamics of the intravenously administered, highly selective EZH2 inhibitor, GSK2816126, (NCT02082977).
GSK126 | GSK2816126A | EZH2 甲基转移酶抑制剂 | TargetMol
GSK126 (GSK2816126A) 是一种 EZH2 甲基转移酶抑制剂 (IC50=9.9 nM)，具有有效性和选择性。 GSK126 具有抗肿瘤活性，可以抑制肿瘤细胞增殖、抑制血管生成。 MAK683 hydrochloride胚胎外胚层发育 (EED) 抑制剂，也是一种高效的 PRC2 抑制剂，可阻断癌细胞增殖（IC50=1.014），在EED Alphascreen， ELISA 和 LC-MS 试验中测得的IC50 值分别为 59，26，89 nM。 EPZ015666 (GSK3235025) 是一种口服有效的 PRMT5 酶活性抑制剂，IC50 …
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