GW779439X-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGW779439XCat.No.:HY-103645CASNo.:551919-98-3分?式:C??H??F?N?分?量:454.45作?靶點:Bacterial;AuroraKinase;Apoptosis作?通路:Anti-infection;CellCycle/DNADamage;Epigenetics;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:31.25mg/mL(68.76mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2005mL11.0023mL22.0046mL5mM0.4401mL2.2005mL4.4009mL10mM0.2200mL1.1002mL2.2005mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.58mM);ClearsolutionBIOLOGICALACTIVITY?物活性GW779439X，吡唑并吡啶類化合物，?種??葡萄球PASTA激酶Stk1抑制劑。GW779439X增強β-內(nèi)酰胺類抗?素對各種MRSA和MSSA的分離株，有的甚?跨越了從耐藥到敏感的斷點。GW779439X?種AURKA抑制劑，可通過caspases3/7誘導(dǎo)細(xì)胞凋亡(apoptosis)。IC50&TargetAuroraAStk1apoptosis體外研究GW779439X(2μM)biochemicallyinhibitsStk1.GW779439X(5μM)potentiatesceftarolineactivityagainstaceftaroline-resistantMRSAstrain.GW779439XisabletopotentiatetheactivityofoxacillinagainstvariousS.aureusisolates,includingbothMRSAandMSSAisolates,butthepotentiationisclearlystrongestinPBP2A-containingstrains[1].GW779439XhasgrowthinhibitioneffectsontheAGP-01cellline(IC50=0.57μM).GW779439X(1μM)significantlyblockSthecellcycleattheG0/G1phaseandsub-G1phase.GW779439X(1μM;72hours;AGP-01cells)significantlydecreasesexpressionlevelsofgenesinvolvedinproliferationprogression(c-MYC,NRAS,andCDC25A)andincreasesexpressionlevelsofgenesinvolvedincellcycleblocking(CDKN1AandTP53)[2.REFERENCES[1].MesquitaFP,etal.Kinaseinhibitorscreeningrevealsaurora-akinaseisapotentialtherapeuticandprognosticbiomarkerofgastriccancer[publishedonlineaheadofprint,2021Jun23].JCellBiochem.2021;10.1002/jcb.30015.[2].SchaenzerAJ,etal.GW779439XandItsPyrazolopyridazineDerivativesInhibittheSerine/ThreonineKinaseStk1andActAsAntibioticAdjuvantsagainstβ-Lactam-ResistantStaphylococcusaureus.ACSInfectDis.2018;4(10):1508-1518.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For