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BIX-01294 3HCl

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Chemical Structure| 1392399-03-9 同义名 : BIX 01294;BIX-01294 trihydrochloride
CAS号 : 1392399-03-9
货号 : A802290
分子式 : C28H41Cl3N6O2
纯度 : 99%+
分子量 : 600.023
MDL号 : MFCD16618384
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Histone Methyltransferase

    G9a, IC50:2.7 μM
描述 BIX-01294 3HCl is a selective inhibitor for G9a Histone Methyltransferase (G9a HMTase) (IC50 = 1.7 μM), that is responsible for dimethylation of lysine 9 at histone 3 (H3K9me2) at several G9a target genes[1]. To a lesser extent, it slightly inhibits HMTase G9a-like protein (GLP) with IC50 of 38 μM, and has no effect on other known histone methyltransferases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to potentiate induce the generation of pluripotent stem cells from somatic cells in vitro. BIX-01294 (5 µM) is also shown to markedly reduced global levels of H3K9 dimethylation at the pronuclear, 2-cell and 4-cell stages of development and resulted in developmental arrest before blastocyst formation. Embryos transiently exposed to BIX-01294 did not establish pregnancy[2]. BIX-01294 treatment reduced proliferation, migration, contractility and global DNA methylation in foetal PASMCs[3]. As a strong autophagy inducer, BIX-01294 also could induce autophagy-associated cell death via EHMT2/G9a dysfunction and intracellular reactive oxygen species production[4].
作用机制 BIX-01294 is a potent inhibitor of H3K9 dimethylation by inhibiting G9a enzymatic activity and reduces H3K9me2 levels at several G9a target genes.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HeLa cells Function assay Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells, IC50=0.059 μM 23656407
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.67mL

0.33mL

0.17mL

8.33mL

1.67mL

0.83mL

16.67mL

3.33mL

1.67mL
参考文献

[1]Liu F, Chen X, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010;53(15):5844-57.

[2]Park KE, Johnson CM, Cabot RA. IVMBIX-01294, an inhibitor of the histone methyltransferase EHMT2, disrupts histone H3 lysine 9 (H3K9) dimethylation in the cleavage-stage porcine embryo. Reprod Fertil Dev. 2012;24(6):813-21.

[3]Yang Q, Lu Z, et al. BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells. Cell Prolif. 2012;45(4):335-44.

[4]Kim Y, Kim YS, et al. BIX-01294 induces autophagy-associated cell death via EHMT2/G9a dysfunction and intracellular reactive oxygen species production. Autophagy. 2013;9(12):2126-39.