SC-514 (354812-17-2) is a reversible, competitive inhibitor of IKK2 (IC50 = 11.2 μM). Has not been demonstrated to inhibit other IKK isoforms, or other kinases. SC-514 displays dose-dependent inhibition of the transcription of NF-κB dependent genes in cell culture.1
A cell-permeable (thienothienyl)amino-acetamide compound that displays anti-inflammatory properties. Acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of IKK-2 (IC50 ~3-12 μM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2). Its specificity has been confirmed using a panel of 31 other kinases, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC50 > 200 μM). Shown to specifically block NF-kB-dependent gene expression, but not MAP kinase pathways, in stimulated synovial fibroblasts RASF.
ChEBI: 3-amino-5-(3-thiophenyl)-2-thiophenecarboxamide is a ring assembly and a member of thiophenes.
1) Kishore et al. (2003), A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts; J. Biol. Chem., 278 32861
