ZT-12-037-01
规格
| Cas Number | 2328073-61-4 |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 简短描述 | 丝氨酸/苏氨酸激酶抑制剂 |
| 英文简短描述 | Serine/threonin kinase Inhibitors |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | ZT-12-037-01 是一种特异性 ATP 竞争性 STK19 抑制剂，对 STK19 (WT) 和 STK19 (D89N) 的 IC50 分别为 23.96 nM 和 27.94 nM。利用 KINOMEscan 对 468 种不同的激酶进行体外 ATP 位点竞争结合试验，它在 1 μM 时显示出极高的激酶选择性。 |
| 英文描述 |
Information ZT-12-037-01 ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM. Targets STK19 (Cell-free assay); STK19 (D89N) (Cell-free assay) 23.96 nM; 27.94 nM In vitro ZT-12-037-01 treatment efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner. Furthermore, with increasing ATP concentrations, the IC50 of ZT-12-037-01 against STK19 accordingly increased, indicating that ZT-12-037-01 is an ATP-competitive inhibitor for STK19. ZT-12-037-01 treatment significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation, proliferation, and tumor formation. Pro-apoptotic effect of ZT-12-037-01 is dramatically enhanced in cells expressing oncogenic NRAS. In vivo ZT-12-037-01 is a highly potent STK19 inhibitor with low in vivo toxicity. Its treatment also inhibits growth of SK-MEL-2 xenograft melanoma (with NRASQ61R) in a dose-dependent manner. Cell Research(from reference) Cell lines：A375, UACC62, SK-MEL-2 and WM2032 cells Concentrations：0 μM, 1 μM, or 3 μM Incubation Time：4 days |