Capzimin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECapziminCat.No.:HY-110404CASNo.:2084868-04-0分⼦式:C₃₀H₂₄N₆O₂S₄分⼦量:628.81作⽤靶点:Proteasome作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥55.67mg/mL(88.53mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5903mL7.9515mL15.9031mL5mM0.3181mL1.5903mL3.1806mL10mM0.1590mL0.7952mL1.5903mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(3.98mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.98mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Capzimin有效的，特异性适中的，蛋⽩酶体异肽酶Rpn11抑制剂。IC50&TargetTarget:Rpn11[1]体外研究Capzimin(3027)shows80-foldselectivityforRpn11overCsn5,10-foldoverAMSHand6-foldoverBRCC36(IC50=30μM,4.5μMand2.3μMrespectively.CapziminisscreenedagainsttheNCIpanelof60cancercelllines.ThemedianGI50is3.3μM.CapziminexhibitspromisingactivityinleukemiacellsincludingtheSRandK562celllines(GI50valuesof0.67μMand1μMrespectively),aswellasseveralsolidtumorcelllinesincludingNCI-H460(non-smallcelllungcancer;GI50=0.7μM)andMCF7(breastcancer;GI50=1.0μM).Immunoblottingfortheprocessedformofcaspase3andcaspase-cleavedpolyADP-ribosepolymeraseinHCT116cellsconfirmthatCapziminnotonlyblockscellgrowth,butalsoinducesapoptosis[1].PROTOCOLKinaseAssay[1]Fluorescencepolarizationassaysareperformedinlow-volume384wellsolidblackplatesinquadruplicate.Theassaysareperformedinbuffercontaining50mMTris-HClpH7.5,1mMMgCl2,50μMATP,1mMDTTand0.01%NP-40.Thecomponentsfortheassayareaddedinthefollowsequence:1)5μLcompound(Capzimin,etal.)(in3%DMSO)atdifferentconcentrations,2)5μLofdilutedhuman26Sproteasome,and3)5μLofsubstrate(3nMUb4-peptideOG).100μMZn(cyclen)2+ispresentinthetitrationreactionfortheexperimentsperformedwithZn(cyclen)2+.Fluorescencepolarizationismeasuredat30°Cwithexcitationat480nmandemissionat520nm.CollecteddataisnormalizedtoDMSOcontrolandfittedtoadose-responsecurvetodeterminetheIC50value[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]HCT116cellsaretreatedwithdifferentconcentrationsof3021orCapziminfor72hoursinnormalorlowserummediumandthenmixedwithCellTiter-Gloreagenttoestimatecellproliferation.MeasuredluminescencevaluesarenormalizedtoDMSOcontrolanddataarefittedtoadose-responseequationtodeterminetheGI50[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•SciImmunol.2021Apr30;6(58):eabe2933.•Prostate.2019Aug;79(11):1304-1315.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].LiJ,etal.CapziminisapotentandspecificinhibitorofproteasomeisopeptidaseRpn11.NatChemBiol.2017May;13(5):486-493.McePdfHeightCaution:Producthas