NF-kappaB Activation Inhibitor VII, CID-2858522 - Calbiochem (C15-1303-895)

General description

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).

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).

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 465.63. Empirical Formula: C₂₈H₃₉N₃O₃. Quality Level: 100. Assay: >. 95% (HPLC). form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze. color: off-white. solubility: DMSO: 100 . mg/mL. shipped in: wet ice. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3.