R-MRT199665-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE(R)-MRT199665Cat.No.:HY-120877A分?式:C??H??N?O?分?量:469.58作?靶點(diǎn):MARK;Salt-inducibleKinase(SIK);AMPK;Apoptosis作?通路:CellCycle/DNADamage;Immunology/Inflammation;Epigenetics;PI3K/Akt/mTOR;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性(R)-MRT199665MRT199665(HY-120877)的異構(gòu)體。MRT199665?種有效的，ATP競(jìng)爭(zhēng)性的，選擇性MARK/SIK/AMPK抑制劑，對(duì)MARK1/MARK2/MARK3/MARK14，AMPKα1/AMPKα2和SIK1/SIK2/SIK3的IC50分別為2/2/3/2nM，10/10nM和110/12/43nM。MRT199665作?于MEF2C激活的?急性髓性??病(AML)細(xì)胞，引起凋亡(apoptosis)。MRT199665抑制SIK底物CRTC3磷酸化(在S370位點(diǎn))。REFERENCES[1].ClarkK,etal.PhosphorylationofCRTC3bythesalt-induciblekinasescontrolstheinterconversionofclassicallyactivatedandregulatorymacrophages.ProcNatlAcadSciUSA.2012Oct16;109(42):16986-91.[2].BrownFC,etal.MEF2CPhosphorylationIsRequiredforChemotherapyResistanceinAcuteMyeloidLeukemia.CancerDiscov.2018Apr;8(4):478-497.[3].HutchinsonLD,etal.Salt-induciblekinases(SIKs)regulateTGFβ-mediatedtranscriptionalandapoptoticresponses.CellDeathDis.2020Jan22;11(1):49.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792ax:021-5370