Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 11 nM against NF-κB transcriptional activation in Jurkat cells; 7 nM against LPS-induced TNF-α production in murine splenocytes

Cell permeable: yes

Primary TargetNF-κB transcriptional activation

General description

A cell-permeable quinazoline compound that acts as a potent inhibitor of NF-κB transcriptional activation (IC₅₀ = 11 nM in Jurkat cells) and LPS-induced TNF-α production (IC₅₀ = 7 nM in murine splenocytes). Does not exhibit cellular cytotoxicity even at concentrations as high as 10 µM. Reported to exhibit anti-inflammatory effects on carregeenin-induced paw edema in rats.

Legal Information

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

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 383.

Packaging

Packaged under inert gas

1 mg in Plastic Bag(s)

Physical form

A 10 mM (1 mg/281 µl) solution of NF-κB Activation Inhibitor (Cat. No. 481406) in DMSO.

Reconstitution

Following initial use, aliquot and refrigerate (4°C).

Warning

Toxicity: Toxic (F)