Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETC13172Cat.No.:HY-101524CASNo.:2093393-05-4分?式:C??H??N?O?S分?量:388.4作?靶點(diǎn):MixedLineageKinase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:25mg/mL(64.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5747mL12.8733mL25.7467mL5mM0.5149mL2.5747mL5.1493mL10mM0.2575mL1.2873mL2.5747mL請(qǐng)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(qǐng)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(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.25mg/mL(5.79mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.25mg/mL(5.79mM);ClearsolutionBIOLOGICALACTIVITY?物活性TC13172MLKL的抑制劑，作?于HT-29細(xì)胞，其EC50值為2nM。IC50&TargetEC50:2±0.6nM(MLKL,inHT-29cells)[1].體外研究Theanti-necroptosispotencyofTC13172isevaluatedintheHT-29cellline,theEC50valueis2±0.6nM.TC13172hasaninhibitionpotencyof2nMagainstcellnecroptosis.TC13172inhibitsMLKLbydirectlybindingtoCys-86.TC13172doesnotdisruptthephosphorylationofMLKL,butdodecreasethelevelofMLKLinthemembranephase,demonstratingthattheseMLKLinhibitorsblockthetranslocationofMLKLtothecellmembrane,therebyprotectingcellsfromnecroptosis[1].PROTOCOLCellAssay[1]Humancolorectaladenocarcinoma(HT)-29cellsareincubatedwithcompound12(1mM)orDMSOfor2h.Forthebindingcompetitionexperimentsamples,cellsarepre-incubatedwith5mMNSAor100nMTC13172for2h,1mMcompound12isthenaddedandincubatedforanadditional2h.Theclickreaction(Biotin-C2H4-N310mM,TBTA10mM,CuSO450mM,Sodiumascorbate50mM)iscarriedoutwithcelllysatesfor2h.ThebiotinmodifiedproteinsareenrichedandanalysedbywesternblottingusingantibodiesagainstflagandGAPDH[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].BoYan,etal.Discoveryofanewclassofhighlypotentnecroptosisinhibitorstargetingthemixedlineagekinasedomain-likeprotein.ChemCommun(Camb).2017Mar28;53(26):3637-3640.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo