c-Jun-N-terminal-kinase抑制剂-激动剂-MCE

(c-JunN-terminalkinases)belongtothemitogen-activatedproteinkinasefamily,andareresponsivetostressstimuli,suchascytokines,ultravioletirradiation,heatshock,andosmoticshock.JNKsplayaroleinTcelldifferentiationandthecellularapoptosispathway.Activationoccursthroughadualphosphorylationofthreonine(Thr)andtyrosine(Tyr)residueswithinaThr-Pro-TyrmotiflocatedinkinasesubdomainVIII.ActivationiscarriedoutbytwoMAPkinases,MKK4andMKK7andJNKcanbeinactivatedbySer/ThrandTyrproteinphosphatases.DownstreammoleculesthatareactivatedbyJNKincludec-Jun,ATF2,ELK1,SMAD4,p53andHSF1.JNKscanassociatewithscaffoldproteinsJNKinteractingproteinsaswellastheirupstreamkinasesJNKK1andJNKK2followingtheiractivation.JNKactivityregulatesseveralimportantcellularfunctionsincludingcellgrowth,differentiation,survivalandapoptosis.Purity:98%ClinicalData:Size:10mMx1mLinDMSO,2mg,5mg,10mg,50mg,100mgPurity:98%ClinicalData:Size:10mMx1mLinDMSO,5mg,10mg,25mg,50mg,100mgPurity:98%ClinicalData:Size:10mMx1mLinDMSO,2mg,5mg,10mg,50mg,100mgPurity:98%ClinicalData:Size:1mg,5mg,10mg,50mgPurity:99.59%ClinicalData:Phase2Size:10mMx1mLinDMSO,2mg,5mg,10mg,50mg,100mgPurity:98.80%ClinicalData:Size:10mMx1mLinDMSO,2mg,5mg,10mg,50mgPurity:98%ClinicalData:Size:2mg,5mg,10mg,50mgPurity:98%ClinicalData:Size:10mMx1mLinDMSO,1mg,5mg,10mg,50mgPurity:98.78%ClinicalData:Size:10mMx1mLinDMSO,5mg,10mg,50mgPurity:98%ClinicalData:Size:10mMx1mLinDMSO,10mg,50mg,100mgJNKInhibitors&ModulatorsBioactivity:Anisomycinisapyrrolidineantibiotic,actsasananti-fungalantibioticwhichinhibitsProteinSynthesis,alsoisapotentactivatorofSAPKs/JNKs.Bioactivity:AS602801(Bentamapimod)isanovel,orallyactiveinhibitorofJNK.Bioactivity:AS601245isaninhibitorofthec-JunNH2-terminalkinase(JNK)(hJNK1:IC50=150nM,hJNK2:IC50=220nMandhJNK3:IC50=70nM),hasneuroprotectiveproperties.Bioactivity:CC-401isasecondgenerationATP-competitiveanthrapyrazolonec-JunNterminalkinase(JNK)inhibitorwithpotentialantineoplasticactivity.Bioactivity:CC-401HclisasecondgenerationATP-competitiveanthrapyrazolonec-JunNterminalkinase(JNK)inhibitorwithpotentialantineoplasticactivity.Bioactivity:CC-930(Tanzisertib)isaselectiveandpotentJNK1/JNK2/JNK3(IC50=61/7/6nM)inhibitorandiscurrentlyunderclinicaldevelopmentforfibroticandinfammatoryindications.Bioactivity:Bioactivity:DB07268isapotentandselectiveJNK1inhibitorwithanIC50valueof9nM.Bioactivity:Bioactivity:JNK-IN-7isarelativelyselectiveJNKsinhibitor(IC50=1.54/1.99/0.75forJNK1/2/3);alsoboundtoIRAK1,PIK3C3,PIP5K3andPIP4K2C.2Tel:[phone]Fax:[phone]Email:[e-mail](Flagecidin;WuningmeisuC)Cat.No.:HY-18982AS602801(Bentamapimod;AS602801;AS-602801)Cat.No.:HY-14761AS601245(AS-601245)Cat.No.:HY-11010CC-401(CC401;CC401)Cat.No.:HY-13022ACC-401hydrochloride (CC401hydrochloride;CC401hydrochloride;CC401HCl)Cat.No.:HY-13022CC-930(Tanzisertib;CC930;CC930)Cat.No.:HY-15495D-JNKI-1(AM-111;XG-102)Cat.No.:HY-P0069DB07268(DB07268;DB-07268)Cat.No.:HY-15737IQ-1Sfreeacid(IQ1Sfreeacid)Cat.No.:HY-100233JNK-IN-7(JNKinhibitor)Cat.No.:HY-15617:Size:10mMx1mLinDMSO,10mg,50mgPurity:98%ClinicalData:Size:10mMx1mLinDMSO,2mg,5mg,10mgPurity:98.80%ClinicalData:Size:10mMx1mLinDMSO,10mg,50mg,100mgPurity:98.95%ClinicalData:Size:10mMx1mLinDMSO,5mg,10mg,50mg Bioactivity:JNK-IN-8isaselectiveJNK1/2/3inhibitor(IC50=4.67/18.7/0.98nM)thatinhibitsphosphorylationofc-Jun,adirectsubstrateofJNK,incellsexposedtosubmicromolardruginamannerthatdependsoncovalentmodificationoftheconservedcysteineresidue.Bioactivity:SP600125isabroad-spectrumJNKinhibitorforJNK1,JNK2andJNK3withIC50of40nM,40nMand90nM,respectively;10-foldgreaterselectivityagainstMKK4,25-foldgreaterselectivityagainstMKK3,MKK6,PKB,andPKC(alpha),and100-foldselectivityagainstERK2,p38,Chk1,EGFRetc.Bioactivity:SR-3306isabrainpenetrantsmallmoleculeJNKinhibitorfromtheaminopyrimidineclass.Bioactivity:TCSJNK5a(JNKInhibitorIX)isaselectiveinhibitorofJNK2andJNK3(pIC50valuesare6.7,6.5,<5.0and<4.8forJNK3,JNK2,JNK1andp38(alpha)respectively);displaysnosignificantactivityatarangeofotherproteinkinasesincludingEGFR,ErbB2,cdk2,JNK-IN-8 ((E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benz…)Cat.No.:HY-13319SP600125(SP600125;SP-600125)Cat.No.:HY-12041SR-3306Cat.No.:HY-12829TCSJNK5a(JNKInhibitorIX)Cat.No.:HY-15881