BIX 01294
| 中文名称 | BIX 01294 |
|---|---|
| 中文同义词 | 2-(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)-6,7-二甲氧基-N-[1-(苯基甲基)-4-哌啶基]-4-喹唑啉胺;2-(HEXAHYDRO-4-METHYL-1H-1,4-DIAZEPIN-1-YL)-6,7-DIMETHOXY-N-[1-(PHENYLMETHYL)-4-PIPERIDINYL]-4-QUINAZOLINAMINE 三盐酸盐 水合物;BIX 01294 三盐酸盐 水合物;N-(1-苄基哌啶-4-基)-6,7-二甲氧基-2-(4-甲基-1,4-二氮杂环庚-1-基)喹唑啉-4-胺;BIX01294游离;BIX 01294,2-(六氢-4-甲基-1H-1,4-二氮杂-1-基)-6,7-二甲氧基-N-[1-(苯基甲基)-4-哌啶基]-4-喹唑啉胺水合三盐酸盐;N-(1-苄基哌啶-4-基)-6,7-二甲氧基-2-(4-甲基-1,4-二氮杂卓-1-基)喹唑啉-4-胺;BIX-01294,G9A和G9A样蛋白组蛋白甲基转移酶抑制剂 |
| 英文名称 | BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride |
| 英文同义词 | 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinaminetrihydrochloride;BIX 01294;BIX 01294 hydrate trihydrochloride;BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride;4-QuinazolinaMine, 2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6,7-diMethoxy-N-[1-(phenylMethyl)-4-piperidinyl]-;2-(Hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6,7-diMethoxy-N-[1-(phenylMethyl)-4-piperidinyl]-4-quinazolinaMine hydrate trihydrochloride;BIX 01294 (free base);2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine |
| CAS号 | 935693-62-2 |
| 分子式 | C28H38N6O2 |
| 分子量 | 490.64 |
| EINECS号 | |
| 相关类别 | 细胞周期;信号转导通路激酶抑制剂;Epigenetics;G9a-like protein and G9a histone lysine methyltransferase (HMTase) inhibitor. |
| Mol文件 | 935693-62-2.mol |
| 结构式 |  |
BIX 01294 性质
| 沸点 | 654.6±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.195±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 可溶于 DMSO（高达 50 mg/ml）或水（高达 50 mg/ml）。 |
| 酸度系数(pKa) | 9.34±0.70(Predicted) |
| 形态 | 类白色固体 |
| 颜色 | 米白色 |
| 稳定性 | DMSO或蒸馏水中的溶液可在-20°下稳定储存3个月。 |
| InChIKey | BZOWJAYUMMHCDW-UHFFFAOYSA-N |
BIX-01294 是一种 G9a 组蛋白甲基转移酶 (G9a Histone Methyltransferase) 抑制剂，IC50 值为 1.9 μM。
IC50: 1.9 μM (G9a Histone Methyltransferase)
BIX-01294 (4.1 μM) treatment of G9anull ES cells results in a further reduction in H3K9me2 levels. BIX-01294 reduces H3K9me2 at several G9a target genes.
BIX-01294 (5 µM) reduces levels of global H3K9 methylation in pronuclear- and 2-cell-stage embryos. Embryos transiently exposed to BIX-01294 have a reduced ability to establish pregnancy.
BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF.