STO-609 acetate

Cat. No. 1551

STO-609 acetate C19H10N2O3.C2H4O2 [1173022-21-3]

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Chemical Name: 7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic acid acetate

Biological Activity

Selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki values are 80 and 15 ng/ml for inhibition of CaM-KKα and CaM-KKβ respectively); competes for the ATP-binding site. Displays > 80-fold selectivity over CaMK1, CaMK2, CaMK4, MLCK, PKC, PKA and p42 MAPK.

Technical Data

M.Wt:
374.35
Formula:
C19H10N2O3.C2H4O2
Solubility:
Soluble to 45 mM in 100mM NaOH and to 10 mM in DMSO with sonication
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
1173022-21-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Tokumitsu et al (2002) STO-609, a specific inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase. J.Biol.Chem. 277 15813. PMID: 11867640.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for STO-609 acetate include:

Horigane et al (2016) Facilitation of axon outgrowth via a Wnt5a-CaMKK-CaMKIα pathway during neuronal polarization. Proc Natl Acad Sci U S A 9 8. PMID: 26772170.

Cohen et al (2015) Evolutionary and functional perspectives on signaling from neuronal surface to nucleus. Mol Brain 460 88. PMID: 25998737.

Lee et al (2015) N-methyl-D-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity. Biochem Biophys Res Commun 8 4. PMID: 25599691.

Obba et al (2015) The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML. Mol Brain 11 1114. PMID: 26029847.

Zhu et al (2015) Adenosine 5'-monophosphate-activated protein kinase regulates IL-10-mediated anti-inflammatory signaling pathways in macrophages. J Exp Med 194 584. PMID: 25512602.

Li et al (2014) Cell cycle-linked MeCP2 phosphorylation modulates adult neurogenesis involving the Notch signalling pathway. Nat Commun 5 5601. PMID: 25420914.

Hutchins et al (2013) Calcium release-dependent actin flow in the leading process mediates axophilic migration. J Neurosci 33 11361. PMID: 23843509.

Iseli et al (2013) Activation of AMPK by bitter melon triterpenoids involves CaMKKβ. PLoS One 8 e62309. PMID: 23638033.

Kim et al (2013) Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation. J Biol Chem 288 22693. PMID: 23754277.

Parker et al (2013) Rapamycin prevents seizures after depletion of STRADA in a rare neurodevelopmental disorder. Sci Transl Med 5 182ra53. PMID: 23616120.

Ashpole et al (2012) Calcium/calmodulin-dependent protein kinase II (CaMKII) inhibition induces neurotoxicity via dysregulation of glutamate/calcium signaling and hyperexcitability. J Biol Chem 287 8495. PMID: 22253441.

Fortin et al (2012) Brain-derived neurotrophic factor activation of CaM-kinase kinase via transient receptor potential canonical channels induces the translation and synaptic incorporation of GluA1-containing calcium-permeable AMPA receptors. J Neurosci 32 8127. PMID: 22699894.

Gaamouch et al (2012) Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity. J Neurosci 32 10767. PMID: 22855824.

Karacosta et al (2012) A regulatory feedback loop between Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) and the androgen receptor in prostate cancer progression. J Biol Chem 287 24832. PMID: 22654108.

Kawashima et al (2012) Ca2+/calmodulin-dependent protein kinase kinase is not involved in hypothalamic AMP-activated protein kinase activation by neuroglucopenia. J Immunol 7 e36335. PMID: 22590531.

Terry et al (2012) Human kinome profiling identifies a requirement for AMP-activated protein kinase during human cytomegalovirus infection. Biochem Biophys Res Commun 109 3071. PMID: 22315427.

Fu et al (2011) Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway. Proc Natl Acad Sci U S A 108 1403. PMID: 21220320.

Fogarty et al (2010) Calmodulin-dependent protein kinase kinase-beta activates AMPK without forming a stable complex: synergistic effects of Ca2+ and AMP. Biochem J 426 109. PMID: 19958286.

Reece et al (2009) The Bα and Bδ regulatory subunits of PP2A are necessary for assembly of the CaMKIV.PP2A signaling complex. J Biol Chem 386 582. PMID: 19538941.

Guire et al (2008) Recruitment of calcium-permeable AMPA receptors during synaptic potentiation is regulated by CaM-kinase I. Mol Cell 28 6000. PMID: 18524905.

Soltoff and Hedden (2008) Regulation of ERK1/2 by ouabain and Na-K-ATPase-dependent energy utilization and AMPK activation in parotid acinar cells. Am J Physiol Cell Physiol 295 C590. PMID: 18632735.

Wayman et al (2008) An activity-regulated microRNA controls dendritic plasticity by down-regulating p250GAP. PLoS One 105 9093. PMID: 18577589.

Göransson et al (2007) Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase. J Biol Chem 282 32549. PMID: 17855357.

Høyer-Hansen et al (2007) Control of macroautophagy by calcium, calmodulin-dependent kinase kinase-β and Bcl-2. Autophagy 25 193. PMID: 17244528.

Reihill et al (2007) AMP-activated protein kinase mediates VEGF-stimulated endothelial NO production. Proc Natl Acad Sci U S A 354 1084. PMID: 17276402.

Sanders et al (2007) Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. Mucosal Immunol 282 32539. PMID: 17728241.

Tamás et al (2006) Regulation of the energy sensor AMP-activated protein kinase by antigen receptor and Ca2+ in T lymphocytes. Biochem Biophys Res Commun 203 1665. PMID: 16818670.

Hawley et al (2005) Calmodulin-dependent protein kinase kinase-beta is an alternative upstream kinase for AMP-activated protein kinase. Cell Metab 2 9. PMID: 16054095.

Guest et al Ca2+/calmodulin-dependent kinase kinase alpha is expressed by monocytic cells and regulates the activation profile. PLoS One 3 e1606. PMID: 18270593.

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Keywords: STO-609 acetate, supplier, Selective, CaM, kinases, inhibitors, inhibits, Ca2+, Binding, Protein, modulators, Calcium, Signaling, Signalling, Calmodulin-Activated, Tocris Bioscience, Calcium Binding Protein Modulator Inhibitor products

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