产品说明
生化/生理作用
BIO-0919278 is a highly selective cyclin-dependent kinase CDK12 inhibitor (Kd = 5.6 μM) with little or no potency against CDK1-7, CDK9, CDK14, CDK16-18 or 344 other kinases (<35% inhibition at 1 μM). BIO-0919278 reduces CDK12-mediated Pol II CTD Ser2 phosphorylation (by 57% at 1 μM; U-2 OS cells) without affecting CDK12-independent Pol II CTD Ser5 phosphorylation, and selectively targets noncanonical NF-κB activation (4-hr 20 ng/mLTWEAK-induced p52 nuclear translocation/NIK mRNA production IC50 = 167/320 nM; U-2 OS cells) without affecting canonical NF-κB activation (TNF-α-stimulated p65 (RelA) nuclear translocation IC50 >30 μM).
基本信息
经验(实验)分子式 | C18H16N4O2 |
分子量 | 320.35 |
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 | 2-8℃ |
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 |
Sigma-Aldrich