TCS PIM-1 1
| 中文名称 | TCS PIM-1 1 |
|---|---|
| 中文同义词 | 3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮;PIM-1激酶抑制剂(TCS PIM-1 1);6-(5-溴-2-羟基苯)-2-氧代-4-苯基-1,2-二氢吡啶-3-腈;化合物TCS PIM-1 1;TCS PIM-1 1,ATP竞争性PIM-1激酶抑制剂 |
| 英文名称 | 3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone |
| 英文同义词 | 3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone;TCS PIM-1 1;SC 204330;6-(5-Bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-3-pyridinecarbonitrile;TCS PIM-1;TCS PIM-1 1, >=98%;SC 204330; TCS PIM 1-1;CS-1482 |
| CAS号 | 491871-58-0 |
| 分子式 | C18H11BrN2O2 |
| 分子量 | 367.2 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;抑制剂;细胞生物学试剂;Inhibitors |
| Mol文件 | 491871-58-0.mol |
| 结构式 |  |
TCS PIM-1 1 性质
| 沸点 | 592.6±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.63±0.1 g/cm3(Predicted) |
| 储存条件 | Store at +4°C |
| 溶解度 | 不溶于水；不溶于乙醇； DMSO 中≥12.8 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 6.93±0.10(Predicted) |
TCS PIM-1 1 (SC 204330)是一种有效的、选择性的 ATP-competitive Pim-1 kianse 抑制剂，其IC50值为50 nM，对 Pim-2 和 MEK1/MEK2 具有良好的选择性（IC50> 20000 nM）。
| Target | Value |
|
Pim1
(Cell-free assay) | 50 nM |
TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-18086 | TCS PIM-1 1 | 5 mg | 627元 | |
| 2024/01/25 | HY-18086 | TCS PIM-1 1 TCS PIM-1 1 | 491871-58-0 | 10mg | 1004元 |