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.

• Synonyme(s) : 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
• Formule empirique (notation de Hill): C₁₉H₁₀N₂O₃ · xC₂H₄O₂
• Numéro CAS: 52029-86-4
• Poids moléculaire : 314.29 (free base basis)
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: yellow
• Solubilité: DMSO: 10 mg/mL; 0.1 M NaOH: 20 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 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)
• Clé InChI: MYKOWOGZBMOVBJ-UHFFFAOYSA-N

Description

Description générale

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).

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Notes préparatoires

May require warming to acheive complete solubilization in DMSO.

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1