STO-609 acetate

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STO-609 acetate | CAS No. 1173022-21-3 | Calcium Binding Protein Modulator Inhibitors
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Description: Selective CaM kinase kinase inhibitor

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

Purity: ≥98%

Product Details
Citations (38)
Reviews (1)

Biological Activity

STO-609 acetate is a 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.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of STO-609 acetate is reviewed on the Chemical Probes website.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Facilitation of axon outgrowth via a Wnt5a-CaMKK-CaMKIalpha pathway during neuronal polarization.
    Horigane S, Ageta-Ishihara N, Kamijo S, Fujii H, Okamura M, Kinoshita M, Takemoto-Kimura S, Bito H
    Mol Brain, 2016;9(1):8.
  2. Glucose deprivation-induced increase in protein O-GlcNAcylation in cardiomyocytes is calcium-dependent.
    Zou L, Zhu-Mauldin X, Marchase R, Paterson A, Liu J, Yang Q, Chatham J
    J Biol Chem, 2012;287(41):34419-31.
  3. COH-SR4 reduces body weight, improves glycemic control and prevents hepatic steatosis in high fat diet-induced obese mice.
    Figarola J, Singhal P, Rahbar S, Gugiu B, Awasthi S, Singhal S
    PLoS ONE, 2013;8(12):e83801.
  4. Adenosine 5'-monophosphate-activated protein kinase regulates IL-10-mediated anti-inflammatory signaling pathways in macrophages.
    Zhu Y, Brown J, Sag D, Zhang L, Suttles J
    J Immunol, 2015;194(2):584-94.
  5. CaMKK beta Is Involved in AMP-Activated Protein Kinase Activation by Baicalin in LKB1 Deficient Cell Lines.
    Ma Y, Yang F, Wang Y, Du Z, Liu D, Guo H, Shen J, Peng H
    PLoS ONE, 2012;7(10):e47900.
  6. Withdrawal of essential amino acids increases autophagy by a pathway involving Ca2+/calmodulin-dependent kinase kinase-beta (CaMKK-beta).
    Ghislat G, Patron M, Rizzuto R, Knecht E
    J Biol Chem, 2012;287(46):38625-36.
  7. STO-609, a specific inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase.
    Tokumitsu et al.
    J.Biol.Chem., 2002;277:15813

Product Datasheets

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Citations for STO-609 acetate

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

38 Citations: Showing 1 - 10

  1. Hepatocyte Growth Factor Regulates Macrophage Transition to the M2 Phenotype and Promotes Murine Skeletal Muscle Regeneration.
    Authors: Choi Et al.
    Front Physiol  2019;10:914
  2. AMP-Activated Protein Kinase Is Essential for the Maintenance of Energy Levels during Synaptic Activation.
    Authors: Marinangeli Et al.
    iScience  2018;9:1
  3. TRPC5-induced autophagy promotes drug resistance in breast carcinoma via CaMKKβ/AMPKα/mTOR pathway.
    Authors: Zhang Et al.
    Sci Rep  2017;7:3158
  4. Pharmacological inhibition of CaMKK2 with the selective antagonist STO-609 regresses NAFLD.
    Authors: York Et al.
    Sci Rep  2017;7:11793
  5. Heterodimers of the transcriptional factors NFATc3 and FosB mediate tissue factor expression for 15(S)-hydroxyeicosatetraenoic acid-induced monocyte trafficking.
    Authors: Kotla Et al.
    J Biol Chem  2017;292:14885
  6. Phosphorylation of p62 by AMP-activated protein kinase mediates autophagic cell death in adult hippocampal neural stem cells.
    Authors: Ha Et al.
    J Biol Chem  2017;292:13795
  7. Direct versus indirect actions of ghrelin on hypothalamic NPY neurons.
    Authors: Hashiguchi
    PLoS One  2017;12(9):e0184261
  8. Facilitation of axon outgrowth via a Wnt5a-CaMKK-CaMKIα pathway during neuronal polarization.
    Authors: Horigane Et al.
    Proc Natl Acad Sci U S A  2016;9:8
  9. Dissection and integration of the autophagy signaling network initiated by bluetongue virus infection: crucial candidates ERK1/2, Akt and AMPK.
    Authors: Lv Et al.
    Sci Rep  2016;6:23130
  10. N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity.
    Authors: Lee Et al.
    Biochem Biophys Res Commun  2015;8:4
  11. Evolutionary and functional perspectives on signaling from neuronal surface to nucleus.
    Authors: Cohen Et al.
    Mol Brain  2015;460:88
  12. Adenosine 5'-monophosphate-activated protein kinase regulates IL-10-mediated anti-inflammatory signaling pathways in macrophages.
    Authors: Zhu Et al.
    J Exp Med  2015;194:584
  13. The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML.
    Authors: Obba Et al.
    Mol Brain  2015;11:1114
  14. Cell cycle-linked MeCP2 phosphorylation modulates adult neurogenesis involving the Notch signalling pathway.
    Authors: Li Et al.
    Nat Commun  2014;5:5601
  15. Activation of AMPK by bitter melon triterpenoids involves CaMKKβ.
    Authors: Iseli Et al.
    PLoS One  2013;8:e62309
  16. Rapamycin prevents seizures after depletion of STRADA in a rare neurodevelopmental disorder.
    Authors: Parker Et al.
    Sci Transl Med  2013;5:182ra53
  17. Calcium release-dependent actin flow in the leading process mediates axophilic migration.
    Authors: Hutchins Et al.
    J Neurosci  2013;33:11361
  18. Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation.
    Authors: Kim Et al.
    J Biol Chem  2013;288:22693
  19. AMPKα1 regulates macrophage skewing at the time of resolution of inflammation during skeletal muscle regeneration.
    Authors: Mounier Et al.
    Cell Metab  2013;18:251
  20. Ca2+/calmodulin-dependent protein kinase kinase is not involved in hypothalamic AMP-activated protein kinase activation by neuroglucopenia.
    Authors: Kawashima Et al.
    J Immunol  2012;7:e36335
  21. 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.
    Authors: Fortin Et al.
    J Neurosci  2012;32:8127
  22. Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity.
    Authors: Gaamouch Et al.
    J Neurosci  2012;32:10767
  23. Calcium/calmodulin-dependent protein kinase II (CaMKII) inhibition induces neurotoxicity via dysregulation of glutamate/calcium signaling and hyperexcitability.
    Authors: Ashpole Et al.
    J Biol Chem  2012;287:8495
  24. A regulatory feedback loop between Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) and the androgen receptor in prostate cancer progression.
    Authors: Karacosta Et al.
    J Biol Chem  2012;287:24832
  25. Human kinome profiling identifies a requirement for AMP-activated protein kinase during human cytomegalovirus infection.
    Authors: Terry Et al.
    Biochem Biophys Res Commun  2012;109:3071
  26. Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway.
    Authors: Fu Et al.
    Proc Natl Acad Sci U S A  2011;108:1403
  27. Calmodulin-dependent protein kinase kinase-beta activates AMPK without forming a stable complex: synergistic effects of Ca2+ and AMP.
    Authors: Fogarty Et al.
    Biochem J  2010;426:109
  28. The Bα and Bδ regulatory subunits of PP2A are necessary for assembly of the CaMKIV.PP2A signaling complex.
    Authors: Reece Et al.
    J Biol Chem  2009;386:582
  29. Ca2+/calmodulin-dependent kinase kinase alpha is expressed by monocytic cells and regulates the activation profile.
    Authors: Guest Et al.
    PLoS One  2008;3:e1606
  30. Regulation of ERK1/2 by ouabain and Na-K-ATPase-dependent energy utilization and AMPK activation in parotid acinar cells.
    Authors: Soltoff and Hedden
    Am J Physiol Cell Physiol  2008;295:C590
  31. Recruitment of calcium-permeable AMPA receptors during synaptic potentiation is regulated by CaM-kinase I.
    Authors: Guire Et al.
    Mol Cell  2008;28:6000
  32. An activity-regulated microRNA controls dendritic plasticity by down-regulating p250GAP.
    Authors: Wayman Et al.
    PLoS One  2008;105:9093
  33. AMP-activated protein kinase mediates VEGF-stimulated endothelial NO production.
    Authors: Reihill Et al.
    Proc Natl Acad Sci U S A  2007;354:1084
  34. Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase.
    Authors: Göransson Et al.
    J Biol Chem  2007;282:32549
  35. Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family.
    Authors: Sanders Et al.
    Mucosal Immunol  2007;282:32539
  36. Control of macroautophagy by calcium, calmodulin-dependent kinase kinase-β and Bcl-2.
    Authors: Høyer-Hansen Et al.
    Autophagy  2007;25:193
  37. Regulation of the energy sensor AMP-activated protein kinase by antigen receptor and Ca2+ in T lymphocytes.
    Authors: Tamás Et al.
    Biochem Biophys Res Commun  2006;203:1665
  38. Calmodulin-dependent protein kinase kinase-beta is an alternative upstream kinase for AMP-activated protein kinase.
    Authors: Hawley Et al.
    Cell Metab  2005;2:9

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Good STO-609 acetate
By Anonymous on 12/05/2021
Species: Mouse

20 microM STO-609 acetate was used to test its effect on MCP1 induced SMC migration.


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