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.
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Synonym(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
Empirical Formula (Hill Notation):
C19H10N2O3 · xC2H4O2
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Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
yellow
solubility
DMSO: 10 mg/mL
0.1 M NaOH: 20 mg/mL
shipped in
ambient
storage temp.
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
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
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.
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
WGK
WGK 1
Certificates of Analysis (COA)
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