E67-2

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。

E67-2 

E67-2 作为 E67 衍生物,是一种低毒、选择性 KIAA1718 Jumonji 结构域抑制剂,其 IC50 值为3.4 µM。E67-2 选择性抑制组蛋白 H3 赖氨酸 9 (H3K9) Jumonji 去甲基化酶,以及组蛋白 H3 赖氨酸 4 (H3K4) 去甲基化酶。

E67-2

E67-2 Chemical Structure

CAS No. : 1364914-62-4

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生物活性

E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase[1].

IC50 & Target

IC50: 3.4 μM (H3K9 Jumonji demethylase)[1]

体外研究
(In Vitro)

E67-2 (1~100 μM; 5 minutes) reduces inhibitory effect against GLP by a factor of approximately 1500, resulting in an IC50 of 75 µM. E67-2 has much reduced inhibition on PHF8 on the doubly methylated H3(1-24)K4me3K9me2 peptide substrate. E67-2 (100~100000 nM; 24 hours; fibroblasts) has significantly reduced cell toxicity [1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

404.55

Formula

C21H36N6O2

CAS 号

1364914-62-4

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]. Upadhyay AK, et al. An analog of BIX-01294 selectively inhibits a family of histone H3 lysine 9 Jumonji demethylases. J Mol Biol. 2012;416(3):319-327.

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