TCS PIM-1 1
| 中文名稱 | TCS PIM-1 1 |
|---|---|
| 中文同義詞 | 3-氰基-4-苯基-6-(3-溴-6-羥基苯基)-2(1H)-吡啶酮;6-(5-溴-2-羥基苯)-2-氧代-4-苯基-1,2-二氫吡啶-3-腈;化合物TCS PIM-1 1;TCS PIM-1 1,ATP競爭性PIM-1激酶抑制劑;化合物TCS PIM-1 1,10 MM DMSO 溶液;PIM-1激酶抑制劑(TCS PIM-1 1);TCS PIM-1 1試劑;TCS PIM-1 1試劑 |
| 英文名稱 | 3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone |
| 英文同義詞 | 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號 | 491871-58-0 |
| 分子式 | C18H11BrN2O2 |
| 分子量 | 367.2 |
| EINECS號 | |
| 相關類別 | 小分子抑制劑;小分子抑制劑，天然產物;抑制劑;Inhibitors;細胞生物學試劑 |
| Mol文件 | 491871-58-0.mol |
| 結構式 |  |
TCS PIM-1 1 性質
| 沸點 | 592.6±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.63±0.1 g/cm3(Predicted) |
| 儲存條件 | Store at +4°C |
| 溶解度 | 不溶于水；不溶于乙醇； DMSO 中≥12.8 mg/mL |
| 形態(tài) | 固體 |
| 酸度系數(pKa) | 6.93±0.10(Predicted) |
| 顏色 | 淺黃至黃色 |
TCS PIM-1 1 (SC 204330)是一種有效的、選擇性的 ATP-competitive Pim-1 kianse 抑制劑，其IC50值為50 nM，對 Pim-2 和 MEK1/MEK2 具有良好的選擇性（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 | 產品編號 | 產品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2025/05/22 | HY-18086 | TCS PIM-1 1 TCS PIM-1 1 | 491871-58-0 | 1 mg | 283元 |
| 2025/05/22 | HY-18086 | TCS PIM-1 1 TCS PIM-1 1 | 491871-58-0 | 10mM * 1mLin DMSO | 507元 |