Description
CAMKK inhibitor
Potent and selective inhibitor of VEGF receptor tyrosine kinase (Flk-1, KDR). Inhibits unactivated kinase 100-fold greater (IC50=0.04 uM) than activated kinase (IC50=4.0 uM)1. Weak inhibitor of PDGF receptor tyrosine kinase (IC50=19.4 uM)2. Inhibits endothelial cell activation and angiogenesis in a mouse model of Alzheimers disease3.
Scientific Background: Selective inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki = 80 and 15 ng/ml for inhibition of CaM-KKalpha and CaM-KKbeta respectively). Binds to the ATP-binding site. Displays >80-fold selectivity over CaMK1, CaMK2, CaMK4, MLCK, PKC, PKA and p42 MAPK. Cell permeable