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Selleckchem/Bentamapimod (AS602801)/S8867

DescriptionBentamapimod(AS602801)isanovel,orallyactiveJNKinhibitorwithIC50valuesof80nM,90nMand230nMforJNK1,JNK2andJNK3respectively.
Targets
JNK1[1](Cell-freeassay)JNK2[1](Cell-freeassay)JNK3[1](Cell-freeassay)
80nM90nM230nM
Invitro

Invitro,AS602801exhibitscytotoxicityagainstbothserum-culturednon-stemcancercellsandcancerstemcellsderivedfromhumanpancreaticcancer,non-smallcelllungcancer,ovariancancerandglioblastomaatconcentrationsthatdoesnotdecreasetheviABIlityofnormalhumanfibroblasts.AS602801alsoinhibitstheself-renewalandtumor-initiatingcapacityofcancerstemcellssurvivingAS602801treatment[2].

Assay
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MethodsTestIndexPMID
Westernblot
Noch-1/p-JNK/activecaspase-3;

PubMed:27655677

Cellsweretreatedasdescribedabove.JNKinhibitorbentamapimodwasaddedincorrespondinggroup.ExpressionofrelevantproteinsincludingphosphorylatedJNK,totalJNKandactivecaspase3proteinswasdetectedwithwesternblotanalysis.GAPDHwasusedasaloADIngcontrol.

27655677
Growthinhibitionassay
Cellviability;

PubMed:27655677

CCK-8assaysidentifiesthatbentamapimodcouldattenuatethrombin-inducedneuronalinjury.Resultsshownarethemean±SEMofrepeatedindependentexperiments.*p<0.001,comparedwithcontrol,one-wayANOVA.

27655677
Invivo

CancerstemcellsinestablishedxenografttumorsarereducedbysystemicadmiNISTrationofAS602801atadoseandschedulethatdidnotadverselyaffectthehealthofthetumor-bearingmice[2].