aladdin 阿拉丁 Z414230 ZT-12-037-01 2328073-61-4 99%

中文名：ZT-12-037-01

英文名：ZT-12-037-01

纯度：≥99%

货号：Z414230

Cas号：2328073-61-4

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

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 NRAS^Q61R) 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 

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