(R)-GSK-3685032

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(R)-GSK-3685032  纯度: 98.02%

(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。

(R)-GSK-3685032

(R)-GSK-3685032 Chemical Structure

CAS No. : 2170140-50-6

规格 价格 是否有货 数量
5 mg ￥5000 In-stock
10 mg ￥8500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

(R)-GSK-3685032 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

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 IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1][2].

IC50 & Target[1]

DNMT1

 

分子量

420.53

Formula

C22H24N6OS
CAS 号

2170140-50-6
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)
溶解性数据
In Vitro: 

DMSO : 60 mg/mL (142.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3780 mL 11.8898 mL 23.7795 mL
5 mM 0.4756 mL 2.3780 mL 4.7559 mL
10 mM 0.2378 mL 1.1890 mL 2.3780 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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