4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
(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。
生物活性
(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 IC 50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
性状
Solid
IC50 & Target[1][2]
DNMT1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 60 mg/mL (142.68 mM; Need ultrasonic)配制储备液