THZ531

产品名称：

THZ531
THZ-5-31-1
THZ 531
(R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide
(2E)-N-[4-[[(3R)-3-[[5-Chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-1-piperidinyl]carbonyl]phenyl]-4-(dimethylamino)-2-butenamide
THZ-531

产品介绍：

产品说明

生化/生理作用

THZ531 is a potent, CDK12/13-selective cyclin-dependent kinase inhibitor (IC50 = 158 nM, 69 nM, 10.5 μM, respectively, against 0.2 ?M CDK12-CycK, CDK13-CycK, CDK9-CycT1; IC50 = 8.5 μM against 25 nM CDK7-CycH-MAT1) that targets CDK12 Cys1039 and CDK13 Cys1017 for irreversible covalent modification while bound to the ATP-binding site, displaying good selectivity over >200 other kinases. THZ531 selectively reduces Pol II CTD Ser2, but not Ser5/Ser7, phosphorylation and transcription activity in Jurkat cultures (200-500 nM), exhibiting antiproliferation potency (IC50 = 50 nM in 72 h) due to time- and dose-dependent apoptosis induction.

基本信息

经验(实验)分子式	C₃₀H₃₂ClN₇O₂
分子量	558.07
MDL编号	MFCD31563595

产品性质

测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	−20℃
SMILES string	CN(C/C=C/C(NC1=CC=C(C=C1)C(N2CCC[C@H](C2)NC3=NC(C4=CNC5=C4C=CC=C5)=C(C=N3)Cl)=O)=O)C

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable