化学信息：
| 化学名 | (3aR)-2-(2-hydroxyphenyl)-3a-methyl-1-[3-(trifluoromethyl)benzoyl]-3,4,6,6a-tetrahydro-2H-pyrrolo[2,3-b]pyrrol-5-one |
|
| 简称 | A-366 | |
| 别名 |
MS-2629, HMS2312E03, AKOS005107865, SMR000126755 |
|
| 中文名 | N/A | |
| 化学式 | C19H27N3O2 | |
| 分子量 | 329.44 | |
| CAS号 | 1527503-11-2 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO65mg/ml; Ethanol65mg/ml |
|
| 溶液配制 | 5mg加入1.52ml DMSO，或者每3.29mg加入1ml DMSO，配制成10mM溶液。SD1092-10mM用DMSO配制。 |
生物信息：
| 产品描述 | A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. | ||||
| 信号通路 | Epigenetics | ||||
| 靶点 | G9a/GLP | － | － | － | － |
| IC50 | 3.3nM | － | － | － | － |
| 体外研究 | A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2. Treatment of various leukemia cell lines in vitro results in marked differentiation and morphological changes of these tumor cell lines. | ||||
| 体内研究 | Treatment of a flank xenograft leukemia model with A-366 results in growth inhibition consistent with the profile of H3K9me2 reduction observed. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | PC-3 prostate adenocarcinoma cells |
| 浓度 | 0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10μM |
| 处理时间 | 72h |
| 方法 | PC-3 prostate adenocarcinoma cells are incubated in triplicate with DMSO or the indicated concentrations of A-366 or UNC0638 for 72 hours. H3K9me2 levels are assessed by In-Cell Western assay. |
| 动物实验 | |
| 动物模型 | SCID-beige female mice (Aml flank xenograft model) |
| 配制 | 98% PEG-400 and 2% Tween-80 |
| 剂量 | 30mg/kg/day |
| 给药方式 | by osmotic mini-pump |
| 产品编号 | 产品名称 | 包装 |
| SD1092-10mM | A-366 (Histone Methyltransferase抑制剂) | 10mM×0.2ml |
| SD1092-5mg | A-366 (Histone Methyltransferase抑制剂) | 5mg |
| SD1092-25mg | A-366 (Histone Methyltransferase抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
