General description

A purine-2,6-dione compound that targets the ATP-binding pocket of B-Raf and effectively inhibits the phosphorylation of MEK by wild-type B-Raf in cell-free in vitro kinase assays (IC₅₀ = 1.7 µM and K_i, app = 106 nM with 100 µM ATP). Reported to be equally potent against the oncogenic V600E B-Raf mutant and exhibit much less activity against PI 3-Kγ (IC₅₀ = 25 µM) and more than 50-fold selectivity over PAK1, GSK-3β, PAK4, MST1, and PIM1 (IC₅₀ ≥ 100 µM).

A purine-2,6-dione compound that targets the ATP-binding pocket of B-Raf and effectively inhibits the phosphorylation of MEK by wild-type B-Raf in cell-free in vitro kinase assays (IC₅₀ = 1.7 µM and K_i, app = 106 nM with 100 µM ATP). Reported to be equally potent against the oncogenic V600E B-Raf mutant and exhibit much less activity against PI 3-Kγ (IC₅₀ = 25 µM) and more than 50-fold selectivity over PAK1, GSK-3β, PAK4, MST1, and PIM1 (IC₅₀ ≥100 µM).

Legal Information

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

Other Notes

Luo, C., et al. 2008. J. Med. Chem.51, 6121.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)