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.

• 別名: 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
• 実験式（ヒル表記法）: C₁₉H₁₀N₂O₃ · xC₂H₄O₂
• CAS番号: 52029-86-4
• 分子量: 314.29 (free base basis)
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: yellow
• 溶解性: DMSO: 10 mg/mL; 0.1 M NaOH: 20 mg/mL
• 輸送温度: ambient
• 保管温度: 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)
• InChI Key: MYKOWOGZBMOVBJ-UHFFFAOYSA-N

詳細

詳細

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).

生物化学的／生理学的作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

調製ノート

May require warming to acheive complete solubilization in DMSO.

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1