STO-609 - CAS 52029-86-4 - Calbiochem

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).

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.

Legal Information

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