BIX-01294 是高度选择性的G9a和GLP组蛋白甲基转移酶可逆抑制剂。它通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP，可诱导坏死性凋亡和自噬，具有抗肿瘤活性。

BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).

BIX-01294 induced caspase-dependent apoptosis in human bladder cancer cells.?BIX-01294 stimulates endoplasmic reticulum stress (ER stress) and up-regulated expression of PMAIP1 through DDIT3 up-regulation.?Furthermore, down-regulation of the deubiquitinase USP9X by BIX-01294 results in downstream reduction of MCL1 expression, leading to apoptosis eventually[1].

On the first day, cells were seeded in 96 well plates.?Twenty-four hours later, BIX-01294 was added at the indicated concentrations in each well.?After treatment by BIX-01294 for another 24 h, we used 10% TCA to immobilize the cells and then evaluated the living cell numbers using the sulforhodamine B assay as previously described[1]

935693-62-2

C28H38N6O2

490.64

DMSO:98 mg/mL (163.33 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years