D-JNKI-1-AM-111-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemED-JNKI-1Cat.No.:HY-P0069CASNo.:1445179-97-4Synonyms:AM-111;XG-102分⼦式:C₁₆₄H₂₈₆N₆₆O₄₀分⼦量:3822.44SequenceShortening:DQSRPVQPFLNLTTPRKPRPPRRRQRRKKRG-NH2作⽤靶点:JNK作⽤通路:MAPK/ERKPathway储存⽅式:Powder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(26.16mM)H2O:≥50mg/mL(13.08mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM0.2616mL1.3081mL2.6161mL5mM0.0523mL0.2616mL0.5232mL10mM0.0262mL0.1308mL0.2616mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE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:≥2.5mg/mL(0.65mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(0.65mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(0.65mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:25mg/mL(6.54mM);Clearsolution;Needultrasonic5.请依序添加每种溶剂：SalineSolubility:50mg/mL(13.08mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性D-JNKI-1(AM-111)⾼效可渗透细胞的JNK抑制剂。序列:Asp-Gln-Ser-Arg-Pro-Val-Gln-Pro-Phe-Leu-Asn-Leu-Thr-Thr-Pro-Arg-Lys-Pro-Arg-Pro-Pro-Arg-Arg-Arg-Gln-Arg-Arg-Lys-Lys-Arg-Gly-NH2。IC50&TargetJNK体外研究D-JNKI-1(AM-111;1μM-1mM)treatmentpreventsapoptosisandlossofneomycin-exposedhaircells[1].体内研究D-JNKI-1(AM-111;10μM)preventsnearlyallhaircelldeathandpermanenthearinglossinducedbyneomycinototoxicityinthescalatympanioftheguineapigcochlea.LocaldeliveryofD-JNKI-1alsopreventsacoustictrauma-inducedpermanenthearinglossinadose-dependentmanner[1].D-JNKI-1(0.3mg/kg,i.p.)reversesthesepathologicaleventsinthebrainmitochondriaoftheratandalmostcompletelyabolishescytochromecreleaseandPARPcleavage[2].D-JNKI-1(1μg/kg,s.c.)resultsinasignificantdecreaseinthediseaseactivityindex,andreducestheexpressionofCD4+andCD8+cellsinmice[3].PROTOCOLAnimalD-JNKI-1isdissolvedina0.9%sodiumchloridesolutionforsubcutaneousapplication.Eachgroup(the1.0%Administration[3]DSSgroupandthe1.5%DSSgroup)israndomlysubdividedintoaninterventiongroup(n=15)andacontrolgroup(n=15).Themiceintheinterventiongroupreceivethreesubcutaneousnuchaladministrationsof1μg/kgD-JNKI-1ondays2,12,and22.Themiceinthecontrolgroupreceivephysiologicalsalinesubcutaneouslyasanegativecontrolatthesametimepointsinacomparablestresssituation.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2020Jan3;11(1):71.•CellRep.2021Feb9;34(6):108736.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Oncotarget.2017Oct6;8(54):92864-92879.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WangJ,etal.Apeptideinhibitorofc-JunN-terminalkinaseprotectsagainstbothaminoglycosideandacoustictrauma-inducedauditoryhaircelldeathandhearingloss.JNeurosci.2003Sep17;23(24):8596-607.[2].ZhaoY,etal.TheJNKinhibitorD-JNKI-1blocksapoptoticJNKsignalinginbrainmitochondria.MolCellNeurosci.2012Mar;49(3):300-10.[3].KerstingS,etal.TheimpactofJNKinhibitorD-JNKI-1inamurinemodelofchroniccolitisinducedbydextransulfatesodium.JInflammRes.2013May3;6:71-81.[4].WangC,etal.Wu-toudecoctionattenuatesneuropathicpainviasuppressingspinalastrocyticIL-1R1/TRAF6/JNKsignaling.Oncotarget.2017Oct6;8(54):92864-92879.McePdfHeight