5-(5,6-Dimethoxybenzimidazol-1-yl)-3-(2-methanesulfonyl-benzyloxy)-thiophene-2-carbonitrile Beige solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A thiophenecarbonitrile compound that acts as a potent ATP-competitive inhibitor of IKK-3 (IKK-e, IC50 = 40 nM) with ~20-fold selectivity over PLK1 and more than 125-fold selectivity over a panel of 9 other commonly studied kinases, including IKK-1/2 (IKK-a/b). Reported to be inactive against cytochrome P450 isozymes (IC50 < 50 µM) 1A2, 2D6, 2C9, and 3A4. Purity: ≥95% by HPLC. Ref.: Bamborough, P., et al. 2006. Bioorg. Med. Chem. Lett. 16, 6236. |
