Biochem/physiol Actions

Target IC₅₀: 120 ng/ml and 40 ng/ml for CaM-KKα and CaM-KKβ isoforms, respectively

Reversible: yes

Product competes with ATP.

Cell permeable: yes

Primary TargetCaM-KKα

General description

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).

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).

Legal Information

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

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.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Preparation Note

May require warming to acheive complete solubilization in DMSO.

Warning

Toxicity: Standard Handling (A)