potent and selective inhibitor of IKK-ε kinase that selectively inhibits IKK-ε with an IC50 value of 40 nM and is essentially inactive at IKK-α and IKK-β
OTAVAchemicals Catalogue Number: 7020402324
CAS Registry Number: 862812-98-4
Purity: 95%+ (HPLC)
Ref.: Bamborough et al. 5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-ε kinase. Bioorganic & Medicinal Chemistry Letters (2006), 16, 6236-6240
Abstract: The identification and hit-to-lead exploration of a novel, potent and selective series of substituted benzimidazole-thiophene carbonitrile inhibitors of IKK-ε kinase is described. A 2-thiophenecarbonitrile (CAS RN 862812-98-4) was identified with an IKK-ε enzyme potency of pIC50 7.4, and has a highly encouraging wider selectivity profile, including selectivity within the IKK kinase family.