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Description

A cell-permeable selective inhibitor of NF-kappaB activation induced by PKC pathway activators such as PMA (IC50 = 70 nM) in a HEK293 cell-based NF-kappaB luciferase reporter gene assay, by operating downstream of PKC but upstream of IKKbeta, without inhibiting other NF-kappaB activation pathways. At 10 µ,M, this compound only inhibits Raf, TLK1, and JAK2 by 57%, 70%, and 53%, respectively, among a panel of 353 protein kinases. In addition, it attenuates CD3/CD28 and PMA/ionomycin-induced production of IL-2 by Jurkat T-cells (IC50<5 µ,M) and anti-IgM-stimulated proliferation of murine B-lymphocytes (IC50 = 2 µ,M).