Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECapziminCat.No.:HY-110404CASNo.:2084868-04-0分?式:C??H??N?O?S?分?量:628.81作?靶點:Proteasome作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥55.67mg/mL(88.53mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5903mL7.9515mL15.9031mL5mM0.3181mL1.5903mL3.1806mL10mM0.1590mL0.7952mL1.5903mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(3.98mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.98mM);ClearsolutionBIOLOGICALACTIVITY?物活性Capzimin有效的，特異性適中的，蛋?酶體異肽酶Rpn11抑制劑。IC50&TargetTarget:Rpn11[1]體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻?SciImmunol.2021Apr30;6(58):eabe2933.?Prostate.2019Aug;79(11):1304-1315.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].LiJ,etal.CapziminisapotentandspecificinhibitorofproteasomeisopeptidaseRpn11.NatChemBiol.2017May;13(5):486-493.McePdfHeightCaution:Producthas