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BIX-01294 trihydrochloride

CAS No. : 1392399-03-9

MCE 站：BIX-01294 trihydrochloride

产品活性：BIX-01294 trihydrochloride 是一种可逆且高度选择性的 G9a 组蛋白甲基转移酶抑制剂，在 DELFIA 试验中的 IC₅₀ 为 2.7 μM。BIX-01294 trihydrochloride 特异性抑制 G9a (H3K9me2) 和 GLP (H3K9me3)，IC₅₀s 分别为 1.7 μM 和 38 μM。BIX-01294 trihydrochloride 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。BIX-01294 trihydrochloride 是一种 (1H-1,4-diazepin-1-yl)-quinazolin-4-yl 胺衍生物，可诱导坏死性凋亡 (necroptosis) 和自噬。BIX-01294 trihydrochloride 在复发性肿瘤细胞中具有抗肿瘤活性。

研究领域：Epigenetics  |  Autophagy

作用靶点：Histone Methyltransferase  |  Autophagy

In Vitro: BIX-01294 (2 μM; 48 h) trihydrochloride selectively inhibits recurrent tumor cell growth.
BIX-01294 (1 μM) trihydrochloride leads to a marked increase in phosphorylation of S345 of MLKL.
BIX-01294 (1 μM) trihydrochloride significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines.
BIX-01294 (1 μM; 6 days) trihydrochloride causes the reduction in H3K9me2 levels in primary and recurrent tumor cells.
BIX-01294 trihydrochloride leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h) trihydrochloride.
BIX-01294 (4.1 μM; for 2 days) trihydrochloride causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 trihydrochloride causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells.
BIX-01294 trihydrochloride has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 trihydrochloride does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM).
BIX-01294 trihydrochloride inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM).
BIX-01294 (1 ?g/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF.

In Vivo: BIX-01294 trihydrochloride (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited.

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