Description General description A cell-permeable and reversible naphthoyl fused benzimidazole compound that acts as a highly selective, potent, ATP-competitive inhibitor of Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK) [IC50 = 120 ng/ml and 40 ng/ml for CaM-KKα and CaM-KKβ isoforms, respectively]. Binds to the catalytic domain of CaM-KK, and inhibits autophosphorylation. Does not significantly affect the activities of CaM-KII, MLCK (IC50 = ~10 µg/ml), CaM-KI, CaM-KIV, PKA, PKC, and p42 MAP kinase (IC50 >10 µg/ml). Has also been reported to inhibit phosphorylation of AMP-activated protein kinase (AMPK). A cell-permeable and reversible napthoyl-fused benzimidazole compound that acts as a highly selective, potent, ATP-competitive inhibitor of Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK) (IC50 = 120 ng/ml and 40 ng/ml for CaM-KKα and CaM-KKβ isoforms, respectively). Reported to bind to the catalytic domain of CaM-KK, and inhibit autophosphorylation. Does not significantly affect the activities of CaM-KII, MLCK (IC50 ~10 µg/ml), CaM-KI, CaM-KIV, PKA, PKC and p42 MAP kinase (IC50 >10 µg/ml). Has also been reported to inhibit phosphorylation of AMP-activated protein kinase (AMPK). Packaging 5 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target CaM-KKα Product competes with ATP. Reversible: yes Target IC50: 120 ng/ml and 40 ng/ml for CaM-KKα and CaM-KKβ isoforms, respectively Packaging Packaged under inert gas Warning Toxicity: Standard Handling (A) Preparation Note May require warming to acheive complete solubilization in DMSO. Other Notes Levine, Y., et al. 2007. J. Biol. Chem.282, 20351. Tokumitsu, H., et al. 2003. J. Biol. Chem.278, 10908. Tokumitsu, H., et al. 2002. J. Biol. Chem.277, 15813.