SML2555

BIO-0919278 racemate

≥98% (HPLC)

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₁₈H₁₆N₄O₂
• CAS Number: 1040706-31-7
• Molecular Weight: 320.35
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: [nH]1c2c([nH][c]1=NC(=O)C(N3Cc4c(cccc4)C3=O)C)cccc2
• InChI key: PWSSISUOJZBZFT-UHFFFAOYSA-N

Description

Biochem/physiol Actions

BIO-0919278 is a highly selective cyclin-dependent kinase CDK12 inhibitor (K_d = 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).

Highly selective CDK12 inhibitor that disrupts noncanonical, but not canonical, NF-κB activation.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable