Synonyms: BIO-0702697 racemate; BIO0702697 racemate; BIO0919278 racemate; Compound 702697 racemate; Compound 919278 racemate; N-(1H-Benzo[d]imidazol-2-yl)-2-(1-oxoisoindolin-2-yl)propenamide; N-1H-Benzimidazol-2-yl-1,3-dihydro-a-methyl-1-oxo-2H-isoindole-2-acetamide
Molecular Formula: C18H16N4O2
Molecular Weight: 320.35
Linear Structural Formula: C18H16N4O2
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: BIO-0919278 is a highly selective cyclin-dependent kinase CDK12 inhibitor (Kd = 5.6 muM) with little or no potency against CDK1-7, CDK9, CDK14, CDK16-18 or 344 other kinases (<35 % inhibition at 1 mum). bio-0919278 reduces cdk12-mediated pol ii ctd ser2 phosphorylation (by 57% at 1 mum; u-2 os cells) without affecting cdk12-independent pol ii ctd ser5 phosphorylation, and selectively targets noncanonical nf-kappab activation (4-hr 20 ng ltweak-induced p52 nuclear translocation ik mrna production ic50="167/320" nm; u-2 os cells) without affecting canonical nf-kappab activation (tnf-alpha-stimulated p65 (rela) nuclear translocation ic50>30 muM).