Non disponible en dehors du Royaume-Uni et de l'Irlande
Biochem/physiol Actions
Reversible: yes
Product competes with ATP.
Primary TargetIKK-2
Target IC50: 18 nM against IKK-2
Cell permeable: yes
General description
A cell-permeable ureidocarboxamido thiophene compound that acts as a potent, reversible, and ATP-competitive inhibitor of IKK-2 (IC50 = 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Further reduces paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg). A 10 mM (500 µg/179 µl) solution of IKK-2 Inhibitor IV (Cat. No. 401484) in DMSO is available.
A cell-permeable, reversible, ATP-competitive, and potent inhibitor of IKK-2 (IC50 = 18 nM) that exhibits selectivity over IKK-1, JNK, and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Shown to reduce paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Podolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther.312, 373.Karin, M., et al. 2004. Nat. Rev. Drug Discov.3, 17.Roshak, A.K., et al. 2002. Inflamm. Res.51, S4.
Packaging
Packaged under inert gas
500 µg in Plastic ampoule
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
Ce produit répond aux critères suivants pour être admissible aux récompenses suivantes :