NF-κB Activation Inhibitor VII, CID-2858522

A cell-permeable selective inhibitor of NF-κB activation induced by PKC pathway activators such as PMA (IC₅₀ = 70 nM) in a HEK293 cell-based NF-κB luciferase reporter gene assay, by operating downstream of PKC but upstream of IKKβ, without inhibiting other NF-κB activation pathways. At 10 µM, 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 µM) and anti-IgM-stimulated proliferation of murine B-lymphocytes (IC₅₀ = 2 µM).

Toxicity: Standard Handling (A)

Peddibhotla, S., et al. 2010. J. Med. Chem.53, 4793.

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