BRD4770 是组蛋白甲基转移酶 G9a 抑制剂。 BRD4770 减少组蛋白 H3 (H3K9) 上赖氨酸 9 的二甲基化和三甲基化，EC50 为 5 μM，对 H3K27me3、H3K36me3、H3K4me3 和 H3K79me3 的影响较小或很小。 BRD4770 可激活共济失调毛细血管扩张症突变 (ATM) 通路并诱导细胞衰老。
| Cas No. | 1374601-40-7 |
| 化学名 | methyl 2-benzamido-1-(3-phenylpropyl)benzimidazole-5-carboxylate |
| Canonical SMILES | COC(=O)C1=CC2=C(C=C1)N(C(=N2)NC(=O)C3=CC=CC=C3)CCCC4=CC=CC=C4 |
| 分子式 | C25H23N3O3 |
| 分子量 | 413.47 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS(pH7.2) (1:2): 0.25 mg/ml,DMSO: 10 mg/ml |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).IC50 value: 5 uM (PANC-1 cell) [1]Target: G9a inhibitorBRD4770 activates the ATM pathway without inducing DNA damage, while the ATR pathway is not affected. BRD4770 is a novel probe for studying G9a and its role in cellular senescence.Treatment of 5 μM BRD4770 for 24 h decreased H3K9 trimethylation level by 23% in PANC-1 cells. BRD9539 also inhibits PRC2 activity. References:
[1]. Yuan Y, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7. |
