D-JNKI-1-AM-111-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemED-JNKI-1Cat.No.:HY-P0069CASNo.:1445179-97-4Synonyms:AM-111;XG-102分?式:C???H???N??O??分?量:3822.44SequenceShortening:DQSRPVQPFLNLTTPRKPRPPRRRQRRKKRG-NH2作?靶點(diǎn):JNK作?通路:MAPK/ERKPathway儲(chǔ)存?式:Powder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(26.16mM)H2O:≥50mg/mL(13.08mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.2616mL1.3081mL2.6161mL5mM0.0523mL0.2616mL0.5232mL10mM0.0262mL0.1308mL0.2616mL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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE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:≥2.5mg/mL(0.65mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(0.65mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(0.65mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:25mg/mL(6.54mM);Clearsolution;Needultrasonic5.請(qǐng)依序添加每種溶劑：SalineSolubility:50mg/mL(13.08mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性D-JNKI-1(AM-111)?效可滲透細(xì)胞的JNK抑制劑。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體外研究D-JNKI-1(AM-111;1μM-1mM)treatmentpreventsapoptosisandlossofneomycin-exposedhaircells[1].體內(nèi)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.戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatCommun.2020Jan3;11(1):71.?CellRep.2021Feb9;34(6):108736.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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