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Sigma-Aldrich

NF-κB Activation Inhibitor VII, CID-2858522

The NF-κB Activation Inhibitor VII, CID-2858522 controls the biological activity of NF-κB. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

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Synonym(s):
NF-κB Activation Inhibitor VII, CID-2858522, 1-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-(2-(3-hydroxypropylamino)-5,6-dimethyl-1H-benzo[d]imidazol-1-yl)ethanone; CID-2858522; 2-aminobenzimidazole; Compound 1a
Empirical Formula (Hill Notation):
C28H39N3O3
Molecular Weight:
465.63
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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

WGK

WGK 3


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