EML741

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EML741 

EML741 是一种组蛋白甲基转移酶 (G9a/GLP) 抑制剂，对 G9a 的 IC50 和 Kd 值分别为 23 nM 和 1.13 μM。EML741 可抑制 DNMT1 (IC50，3.1 μM)，但对 DNMT3a 或 DNMT3b 无作用。EML741 具有低细胞毒性，同时表现出良好的膜透过性和血脑屏障透过性。

EML741

EML741 Chemical Structure

CAS No. : 2328074-38-8

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生物活性

EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated[1].

IC50 & Target[1]

G9a

23 nM (IC50)

GLP

 

G9a

1.13 μM (Kd)

DNMT1

3.1 μM (IC50)

体外研究
(In Vitro)

EML741 (Compound 12a) shows a similar high inhibition potency against G9a (97%, 98% inhibition at 10 μM and 25 μM, respectively) and GLP (95%, 98% inhibition at 10 μM and 25 μM, respectively)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

523.75

Formula

C31H49N5O2
CAS 号

2328074-38-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Milite, et al. Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. J Med Chem. 2019 Mar 14;62(5):2666-2689.

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