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ZT-12-037-01
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ZT-12-037-01图片
CAS NO:2328073-61-4

ZT-12-037-01 是靶向选择性丝氨酸/苏氨酸激酶 STK19 抑制剂，与 STK19 蛋白具有高亲和力相互作用，抑制 NRAS 驱动的黑素细胞恶性转化。ZT-12-037-01 是ATP 竞争性抑制剂，可以抑制 NRAS 的磷酸化，IC50 为24 nM。
Cas No.2328073-61-4
Canonical SMILESCOC1=CC2=NC(NC3CC3)=NC(NC4CCN(C(C)C)CC4)=C2C=C1OC
分子式C21H31N5O2
分子量385.5
溶解度DMSO: 8.33 mg/mL (21.61 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 IC50 of 24 nM[1].

ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation[1].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[1]. Cell Proliferation Assay[1] Cell Line: CDK4 (R24C) melanocyte cells; hTERT melanocyte cells; p53DD melanocyte cells

ZT-12-037-01 (injection subcutaneously; 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[1]. Animal Model: SK-MEL-2 xenograft melanoma nude mice with hTERT/p53DD/CDK4(R24C) melanocytes[1]

[1]. Yin C, et al. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16.

 
 
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