Biochem/physiol Actions

Kd = 2.4 nM for B-raf

Reversible: yes

Product competes with ATP.

Primary TargetRaf Kinase

Cell permeable: yes

General description

A cell-permeable triarylimidazole compound that acts as a reversible, ATP-competitive, and highly potent inhibitor of Raf kinase (IC₅₀ = 10 nM & K_d = 2.4 nM for B-raf) with 7-, 30-, and 70-fold selectivity over p38α, GSK-3β, and Lck, respectively. Cellular data have indicated that the compound is more effective towards Raf-1and A-Raf than B-Raf.

A cell-permeable triarylimidazole compound that acts as a reversible, ATP-competitive, and highly potent inhibitor of Raf kinase (IC₅₀ = 10 nM and K_d = 2.4 nM for B-raf) with 7-, 30-, and 70-fold selectivity over p38α, GSK-3β, and Lck, respectively. Cellular data have indicated that the compound is more effective towards Raf-1and A-Raf than B-Raf.

Legal Information

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

Other Notes

Takle, A.K., et al. 2006. Bioorg. Med. Chem. Lett.16, 378.Shelton, J.G., et al. 2003. Leukemia17, 1765.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Warning

Toxicity: Irritant (B)