TC13172-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETC13172Cat.No.:HY-101524CASNo.:2093393-05-4分⼦式:C₁₇H₁₆N₄O₅S分⼦量:388.4作⽤靶点:MixedLineageKinase作⽤通路:MAPK/ERKPathway储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(64.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5747mL12.8733mL25.7467mL5mM0.5149mL2.5747mL5.1493mL10mM0.2575mL1.2873mL2.5747mL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%salineSolubility:≥2.25mg/mL(5.79mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.25mg/mL(5.79mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TC13172MLKL的抑制剂，作⽤于HT-29细胞，其EC50值为2nM。IC50&TargetEC50:2±0.6nM(MLKL,inHT-29cells)[1].体外研究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