General description
A cell-permeable triarylimidazole compound that acts as a reversible, ATP-competitive, and highly potent inhibitor of Raf kinase (IC50 = 10 nM & Kd = 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 Kd = 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.
Biochem/physiol Actions
Cell permeable: yes
Kd = 2.4 nM for B-raf
Primary Target
Raf Kinase
Product competes with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Other Notes
Takle, A.K., et al. 2006. Bioorg. Med. Chem. Lett.16, 378.
Shelton, J.G., et al. 2003. Leukemia17, 1765.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 553014-1MG