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.
BIX-01294 3HCl 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
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