BIX-01294 trihydrochloride是一种G9a histone methyltransferase抑制剂，无细胞试验中IC₅₀为2.7 μM，降低大部分组蛋白H3K9me2，也微弱抑制GLP（主要是H3K9me3），对其他组蛋白甲基转移酶没有显著的抑制活性。

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

BIX 01294

DMSO： 90 mg/mL ； Water： 90 mg/mL

G9a

BIX01294 is a selective inhibitor of G9a histone methyltransferase and does not affect SUV39H1(H320R) and PRMT1 within the tested concentration range. BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1.

[1] Kubicek S, et al. Mol Cell, 2007, 25(3), 473-481.

[2] Imai K, et al. J Biol Chem, 2010, 285(22), 16538-16545.