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CAS No.: 1392399-03-9

BIX-01294 3HCl/BIX 01294三盐酸盐 Catalog No. CSN15913

Synonyms: BIX-01294;BIX01294 HCl

BIX-01294 3HCl is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EHMT2

IC50:2.7μM
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
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
HeLa cells - Function assay - Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells, IC50=0.059 μM 23656407
动物研究
剂量
Mice: 50 mg/kg - 100 mg/kg^[5] (p.o.)

给药途径
p.o.
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HeLa cells	-	Function assay	-	Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells, IC50=0.059 μM	23656407

动物研究
剂量	Mice: 50 mg/kg - 100 mg/kg^[5] (p.o.)
给药途径	p.o.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6666 mL
- 8.3331 mL
- 16.6661 mL
- 5 mM
- 0.3333 mL
- 1.6666 mL
- 3.3332 mL
- 10 mM
- 0.1667 mL
- 0.8333 mL
- 1.6666 mL

技术信息

CAS号

1392399-03-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H41Cl3N6O2

运输

蓝冰

分子量

600.02

别名

BIX-01294;BIX01294 HCl

溶解度

DMSO	90.0 mg/mL (150.0 mM)
Water	90.0 mg/mL (150.0 mM)
Ethanol	90.0 mg/mL (150.0 mM)

动物实验配方

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BIX-01294 3HCl/BIX 01294三盐酸盐 Catalog No. CSN15913

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