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 |