Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDMX-5804Cat.No.:HY-111754CASNo.:2306178-56-1分?式:C??H??N?O?分?量:361.39作?靶點(diǎn):MAP4K作?通路:MAPK/ERKPathway儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(345.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7671mL13.8355mL27.6709mL5mM0.5534mL2.7671mL5.5342mL10mM0.2767mL1.3835mL2.7671mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)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(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.76mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.76mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.76mM);ClearsolutionBIOLOGICALACTIVITY?物活性DMX-5804?種有效、可?服、選擇性的MAP4K4抑制劑，對?MAP4K4的IC50值為3nM，pIC50值為8.55；對MINK1/MAP4K6(pIC50，8.18)和TNIK/MAP4K7(pIC50，7.96)的作?相對較弱。DMX-5804能夠增強(qiáng)?肌細(xì)胞存活率，減少??的缺?再灌注損傷[1]。IC50&TargetMAP4K4MAP4K4MINK1/MAP4K6TNIK/MAP4K73nM(IC50)8.55(pIC50)8.18(pIC50)7.96(pIC50)GCK/MAP4K2KHS/MAP4K5GLK/MAP4K3MLK1/MAP3K96.50(pIC50)6.36(pIC50)4.95(pIC50)7.19(pIC50)MLK3/MAP3K11NUAKVEGFRABL16.99(pIC50)6.88(pIC50)5.72(pIC50)5.80(pIC50)AuroraBFLT3GSK3β5.49(pIC50)5.31(pIC50)4.66(pIC50)體外研究DMX-5804exhibitsgreatselectivityatMAP4K4overotherkinases,suchasGCK/MAP4K2(pIC50,6.50),GLK/MAP4K3(pIC50,4.95),KHS/MAP4K5(pIC50,6.36),ABL1(pIC50,5.80),AuroraB(pIC50,5.49),FLT3(pIC50,5.31),GSK3β(pIC50,4.66),MLK1/MAP3K9(pIC50,7.19),MLK3/MAP3K11(pIC50,6.99),NUAK(pIC50,6.88)andVEGFR(pIC50,5.72)[1].REFERENCES[1].FiedlerLR,etal.MAP4K4InhibitionPromotesSurvivalofHumanStemCell-DerivedCardiomyocytesandReducesInfarctSizeInVivo.CellStemCell.2019Mar1.pii:S1934-5909(19)30013-X.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse