570250

STO-609

A cell-permeable and reversible naphthoyl fused benzimidazole compound that acts as a highly selective, potent, ATP-competitive inhibitor of Ca²⁺/CaM-KK.

• Sinónimos: STO-609, 7H-Benz[de]benzimidazo[2,1-a]isoquinoline-7-one-3-carboxylic Acid, Acetate, 7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic Acid, Acetate
• Fórmula empírica (notación de Hill): C₁₉H₁₀N₂O₃ · xC₂H₄O₂
• Número de CAS: 52029-86-4
• Peso molecular: 314.29 (free base basis)
• Código UNSPSC: 12352200

Propiedades

• Nivel de calidad: 100
• Análisis: ≥95% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; desiccated (hygroscopic); protect from light
• color: yellow
• solubilidad: DMSO: 10 mg/mL; 0.1 M NaOH: 20 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C19H10N2O3/c22-18-13-5-3-4-10-11(19(23)24)8-9-12(16(10)13)17-20-14-6-1-2-7-15(14)21(17)18/h1-9H,(H,23,24)
• Clave InChI: MYKOWOGZBMOVBJ-UHFFFAOYSA-N

Descripción

Descripción general

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).

Acciones bioquímicas o fisiológicas

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

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Nota de preparación

May require warming to acheive complete solubilization in DMSO.

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 1