ChemicalName: | 4-hydroxy-3-(2"-hydroxy-[1,1"-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile |
MolecularWeight: | 360.39 |
Formula: | C20H12N2O3S |
Purity: | ≥98% |
CAS#: | 844499-71-4 |
Solubility: | DMSOupto50mM |
Storage: | Powder:4oC1yearDMSO:4oC3month-20oC1year |
A769662isapotentandselectivesmall-moleculeactivatorofAMP-activatedproteinkinase(AMPK).ItinducesallostericactivationofAMPKandinhibitionofdephosphorylationofAMPKonThr-172,similartotheeffectsofAMP.TheactivationofAMPKinhibitsmTORsignaling,whichisapositiveeffectorofcellgrowthandsurvival.A769662stimulatedpartiallypurifiedratliverAMPKwithanEC50of0.8µMandinhibitedfattyacidsynthesisinprimaryrathepatocyteswithanIC50of3.2µM.ItcanalsostimulateNa+,K+-ATPaseactivityinskeletalmusclecells.
HowtoUse:
Invitro:A769662istypicallyusedat10-20µMconcentrationinvitro.
Invivo:A769662couldbeintraperitoneally(IP)dosedtomiceat30mg/kgtwiceperday.
Reference:
- 1.CoolB,etal.IdentificationandcharacterizationofasmallmoleculeAMPKactivatorthattreatskeycomponentsoftype2diabetesandthemetabolicsyndrome.(2006)CellMetab.3:403-416.
- 2.ScottJW,etal.ThienopyridonedrugsareselectiveactivatorsofAMP-activatedproteinkinaseβ1-containingcomplexes.(2008)Chem.Biol.15:1220-1230.
- 3.HuangX,etal.ImportantroleoftheLKB1-AMPKpathwayinsuppressingtumOrigenesisinPTEN-deficientmice.(2008)BiochemJ.412:211-221.
- 4.MorizaneY,etal.AMP-activatedproteinkinasesuppressesmatrixmetalloproteinase-9expressioninmouseembryonicfibroblasts.(2011)JBiolChem.286(18):16030-8.
- 5.BenzianeB,etal.ActivationofAMP-activatedproteinkinasestimulatesNa+,K+-ATPaseactivityinskeletalmusclecells.(2012)JBiolChem.287(28):23451-63.
A769662_spec.pdf
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