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Potent,selectivelactatedehydrogenaseA(LDHA)inhibitor(IC50valuesare1.9and14nMforLDHAandLDHBrespectively).Inhibitslactateproductioninselectedcancercelllines.ReducesglucoseuptakeandenhancesmitochondrialoxygenconsumptioninSnu398hepatocellularcarcinomacells.InhibitsproliferationandinducesapoptosisinSnu398cells.Inhibitstranscriptionofhistone2B(H2B)geneinHCT116andNCM460cells.Cellpermeable.
SoldforresearchpurposesunderagreementfromGlaxoSmithKline.
GSK2837808AisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight649.62.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Billiardetal(2013)Quinoline3-sulfonamidesinhibitlactatedehydrogenaseAandreverseaerobicglycolysisincancercells.CancerMetab.119PMID:24280423
Xieetal(2014)Targetinglactatedehydrogenase-AinhibitstumOrigenesisandtumorprogressioninmousemodelsoflungcancerandimpactstumor-initiatingcells.Cell.Metab.19795PMID:24726384
Keywords:GSK2837808A,supplier,GSK2837808A,potent,selective,lactate,dehydrogenase,A,LDHA,inhibitors,inhibits,H2B,transcription,Lactate,Dehydrogenase,A,Lactate,Dehydrogenase,A,TocrisBioscience
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