EML741

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EML741

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2328074-38-8

EML741 是一种组蛋白甲基转移酶 (G9a/GLP) 抑制剂，对 G9a 的IC₅₀和K_d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。

生物活性

EML741 is a histone lysine methyltransferaseG9a/GLPinhibitor, with anIC₅₀of 23 nM,K_dof 1.13 μM for G9a. EML741 also inhibitsDNMT1(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)

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].

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.