(R)-GSK-3685032 是 GSK-3685032 的 R 型异构体。GSK-3685032 是一种非时间依赖性、非共价、可逆的 DNMT1 选择性抑制剂，IC50=0.036 μM。GSK-3685032 诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。
货号:ajcx37176
CAS:2170140-50-6
分子式:C22H24N6OS
分子量：420.53
溶解度:DMSO : 60 mg/mL (142.68 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1][2].

[1]. Adams, Nicholas David, et al. Substituted pyridines as inhibitors of DNMT1 and their preparation. WO2017216727A1.
[2]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017.