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Submit ReviewSTO-609 acetate
说明： Selective CaM kinase kinase inhibitor
化学名： 7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic acid acetate
纯度： ≥98% (HPLC)
生物活性 for STO-609 acetate
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.
技术数据 for STO-609 acetate
| 分子量 | 374.35 |
| 公式 | C19H10N2O3.C2H4O2 |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1173022-21-3 |
| PubChem ID | 16760660 |
| InChI Key | WNRSTFUVBWNELX-UHFFFAOYSA-N |
| Smiles | CC(O)=O.OC(=O)C1=C2C=CC=C3C(=O)N4C5=CC=CC=C5N=C4C(C=C1)=C23 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for STO-609 acetate
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 100mM NaOH | 16.85 | 45 | |
| DMSO | 3.74 | 10 超声处理 |
制备储备液 for STO-609 acetate
以下数据基于产品分子量 374.35。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.45 mM | 5.94 mL | 29.68 mL | 59.36 mL |
| 2.25 mM | 1.19 mL | 5.94 mL | 11.87 mL |
| 4.5 mM | 0.59 mL | 2.97 mL | 5.94 mL |
| 22.5 mM | 0.12 mL | 0.59 mL | 1.19 mL |
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产品说明书 for STO-609 acetate
参考文献 for STO-609 acetate
参考文献是支持产品生物活性的出版物。
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 STO-609 acetate, please let us know.
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关键词: STO-609 acetate, STO-609 acetate supplier, Selective, CaM, kinases, inhibitors, inhibits, Ca2+, Binding, Protein, modulators, Calcium, Signaling, Signalling, Calmodulin-Activated, Kinase, 1551, Tocris Bioscience
38 篇 STO-609 acetate 的引用文献
引用文献是使用了 Tocris 产品的出版物。 STO-609 acetate 的部分引用包括：
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
Wayman et al (2008) An activity-regulated microRNA controls dendritic plasticity by down-regulating p250GAP. PLoS One 105 9093 PMID: 18577589
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
Hashiguchi (2017) Direct versus indirect actions of ghrelin on hypothalamic NPY neurons. PLoS One 12 e0184261 PMID: 28877214
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
Iseli et al (2013) Activation of AMPK by bitter melon triterpenoids involves CaMKKβ. PLoS One 8 e62309 PMID: 23638033
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
Choi et al (2019) Hepatocyte Growth Factor Regulates Macrophage Transition to the M2 Phenotype and Promotes Murine Skeletal Muscle Regeneration. Front Physiol 10 914 PMID: 31404148
York et al (2017) Pharmacological inhibition of CaMKK2 with the selective antagonist STO-609 regresses NAFLD. Sci Rep 7 11793 PMID: 28924233
Zhang et al (2017) TRPC5-induced autophagy promotes drug resistance in breast carcinoma via CaMKKβ/AMPKα/mTOR pathway. Sci Rep 7 3158 PMID: 28600513
Lv et al (2016) Dissection and integration of the autophagy signaling network initiated by bluetongue virus infection: crucial candidates ERK1/2, Akt and AMPK. Sci Rep 6 23130 PMID: 26976147
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
Lee et al (2015) N-MthD.-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
Cohen et al (2015) Evolutionary and functional perspectives on signaling from neuronal surface to nucleus. Mol Brain 460 88 PMID: 25998737
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
Mounier et al (2013) AMPKα1 regulates macrophage skewing at the time of resolution of inflammation during skeletal muscle regeneration. Cell Metab 18 251 PMID: 23931756
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
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
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
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
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
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
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
Marinangeli et al (2018) AMP-Activated Protein Kinase Is Essential for the Maintenance of Energy Levels during Synaptic Activation. iScience 9 1 PMID: 30368077
Ha et al (2017) Phosphorylation of p62 by AMP-activated protein kinase mediates autophagic cell death in adult hippocampal neural stem cells. J Biol Chem 292 13795 PMID: 28655770
Kotla et al (2017) Heterodimers of the transcriptional factors NFATc3 and FosB mediate tissue factor expression for 15(S)-hydroxyeicosatetraenoic acid-induced monocyte trafficking. J Biol Chem 292 14885 PMID: 28724635
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
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
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
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
Guest et al (2008) Ca2+/calmodulin-dependent kinase kinase alpha is expressed by monocytic cells and regulates the activation profile. PLoS One 3 e1606 PMID: 18270593
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
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Use in smooth muscle.
By
Mohammad Alqudah on 10/19/2022
分析类型： In Vitro
种属： Rat
细胞系/组织： Smooth muscle
10 uM of STO-609 30 min before challenging smooth muscle strips with contractile agonist in an organ bath.Good inhibition at 10 min the inhibition was minimal.
