ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC 50 of 24 nM.
性状
Solid
体外研究(In Vitro)
ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation.ZT-12-037-01 (0-3 μM) has an inhibitory effects of ZT-12-037-01 on STK19WT and STK19D89N-activated NRAS phosphorylation in HPMs. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
ZT-12-037-01 (intraperitoneally injection; 25-50 mg/kg; once daily; 21 days) inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yin C, et al. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16.
溶解度数据
In Vitro: DMSO : 8.33 mg/mL (21.61 mM; Need ultrasonic)配制储备液