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Medchemexpress/CHIR-99021(Synonyms: CT99021)/HY-10182/100mg
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Medchemexpress/CHIR-99021(Synonyms: CT99021)/HY-10182/100mg
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HY-10182-10mM*1mLinDMSO
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CHIR-99021isaGSK-3α/βinhibitorwithIC50of10nM/6.7nM;>500-foldselectivityforGSK-3versusitsclosesthomologsCDC2andERK2,aswellasotherproteinkinases.

CustomerValidation

  • •NatMed.2016May;22(5):547-56.
  • •MolCell.2017Mar2;65(5):873-884.e8.
  • •CellSignal.2016Mar;28(3):148-56.
  • •Toxicology.2016May20;355-356:31-38.
  • •EnvironToxicol.2017Oct;32(10):2316-2322.
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

CHIR-99021isaGSK-3α/βinhibitorwithIC50of10nM/6.7nM;>500-foldselectivityforGSK-3versusitsclosesthomologsCDC2andERK2,aswellasotherproteinkinases.

IC50&Target

IC50:10nM/6.7nM(GSK-3α/β)[1]

InVitro

CHIR99021inhibitshumanGSK-3βwithKivaluesof9.8nM[1].CHIR99021isasmallorganicmoleculethatinhibitsGSK3αandGSK3βbycompetingfortheirATP-bindingsites.InvitrokinaseassaysrevealthatCHIR99021specificallyinhibitsGSK3β(IC50=~5nM)andGSK3α(IC50=~10nM),withlittleeffectonotherkinases[2].InthepresenceofCHIR-99021theviABIlityoftheES-D3cellsisreducedby24.7%at2.5μM,56.3%at5μM,61.9%at7.5μMand69.2%at10μMCHIR-99021withanIC50of4.9μM[3].

InVivo

InZDFrats,asingleoraldoseofCHIR99021(16mg/kgor48mg/kg)rapidlylowersplasmaglucose,withamaximalreductionofnearly150mg/dl3-4hafteradmiNISTration[1].CHIR99021(2mg/kg)givenonce,4hbeforeirrADIation,significantlyimprovessurvivalafter14.5GyaBDominalirradiation(ABI).CHIR99021treatmentsignificantlyblockscryptapoptosisandaccumulationofp-H2AX+cells,andimprovescryptregenerationandvillusheight.CHIR99021treatmentincreasesLgr5+cellsurvivalbyblockingapoptosis,andeffectivelypreventsthereductionofOlfm4,Lgr5andCD44asearlyas4h[4].

References

  • [1].RingDB,etal.Selectiveglycogensynthasekinase3inhibitorspotentiateinsulinactivationofglucosetransportandutilizationinvitroandinvivo.Diabetes.2003Mar;52(3):588-95.

    [2].BennettCN,etal.RegulationofWntsignalingduringAdipogenesis.JBiolChem.2002Aug23;277(34):30998-1004.

    [3].NaujokO,etal.CytotoxicityandactivationoftheWnt/beta-cateninpathwayinmouseembryonicstemcellstreatedwithfourGSK3inhibitors.BMCResNotes.2014Apr29;7:273.

    [4].WangX,etal.Pharmacologicallyblockingp53-dependentapoptosisprotectsintestinalstemcellsandmicefromradiation.SciRep.2015Apr10;5:8566.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.1490mL10.7448mL21.4897mL
5mM0.4298mL2.1490mL4.2979mL
10mM0.2149mL1.0745mL2.1490mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

KinasesarepurifiedfromSF9cellsthroughuseoftheirHisorGlutag.Glu-taggedproteinsarepurified,andHis-taggedproteinsarepurified.Kinaseassaysareperformedin96-wellplateswithappropriatepeptidesubstratesina300-μLreactionbuffer(variationson50mMTris-HCl,pH7.5,10mMMgCl2,1mMEGTA,1mMdithiothreitol,25mMβ-glycerophosphate,1mMNaF,and0.01%bovineserumalbumin).PeptideshasKmvaluesfrom1to100μM.CHIR99021orCHIRGSKIAisaddedin3.5μLofMe2SO,followedbyATPtoafinalconcentrationof1μM.Afterincubation,triplicate100-μLaliquotsaretransferredtoCombiplate8platescontaining100μL/wellof50μMATPand20mMEDTA.After1hour,thewellsarerinsedfivetimeswithphosphate-bufferedsaline,filledwith200μLofscintillationfluid,sealed,andcountedinascintillationcounter30minlater.Allofthestepsareatroomtemperature.Thepercentageofinhibitioniscalculatedas100×(inhibitor-noenzymecontrol)/(Me2SOcontrol-noenzymecontrol)[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[3]

CHIR99021isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse[3].

TheviabilityofthemouseEScellsisdeterminedafterexposuretodifferentconcentrationsofGSK3inhibitorsforthreedaysusingtheMTTassay.ThedecreaseofMTTactivityisareliablemetabolism-basedtestforquantifyingcellviability;thisdecreasecorrelateswiththelossofcellviability.2,000cellsareseededovernightongelatine-coated96-wellplatesinLIF-containingEScellmedium.OnthenextdaythemediumischangedtomediumdevoidofLIFandwithreducedserumandsupplementedwith0.1-1μMBIO,or1-10μMSB-216763,CHIR-99021orCHIR-98014.BasalmediumwithoutGSK3inhibitorsorDMSOisusedascontrol.Alltestedconditionsareanalyzedintriplicates[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1][4]

CHIR99021isformulatedassolutionsin20mMcitrate-buffered15%CaptisolorasfinesUSPensionsin0.5%carboxymethylcellulose(Rat)[1].
CHIR99021ispreparedinDMSOanddiluted(Mice)[4].

Rat[1]
PrimaryhepatocytesfrommaleSpragueDawleyratsthatweighed<140 g="" are="" prepared="" and="" used="" 1-3="" h="" after="" isolation.="" aliquots="" of="">6cellsin1mLofDMEM/F12mediumplus0.2%BSAandCHIR99021(orallyat16or48mg/kg)orcontrolsareincubatedin12-wellplatesonalow-speedshakerfor30minat37°CinaCO2-enrichedatmosphere,collectedbycentrifugationandlysedbyfreeze/thawinbufferAplus0.01%NP40;theGSassayisagainperformed.
Mice[4]
Mice6-10weeksoldareused.ThePUMA+/+andPUMA-/-littermatesonC57BL/6background(F10)andLgr5-EGFP(Lgr5-EGFP-IRES-creERT2)micearesubjectedtowholebodyirradiation(TBI),orabdominalirradiation(ABI).Miceareinjectedintraperitoneally(i.p.)with2mg/kgofCHIR990214hbeforeradiationor1mg/kgofSB41528628hand4hbeforeradiation.Micearesacrificedtocollectsmallintestinesforhistologyanalysisandwesternblotting.Allmiceareinjectedi.p.with100mg/kgofBrdUbeforesacrifice.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].RingDB,etal.Selectiveglycogensynthasekinase3inhibitorspotentiateinsulinactivationofglucosetransportandutilizationinvitroandinvivo.Diabetes.2003Mar;52(3):588-95.

    [2].BennettCN,etal.RegulationofWntsignalingduringadipogenesis.JBiolChem.2002Aug23;277(34):30998-1004.

    [3].NaujokO,etal.CytotoxicityandactivationoftheWnt/beta-cateninpathwayinmouseembryonicstemcellstreatedwithfourGSK3inhibitors.BMCResNotes.2014Apr29;7:273.

    [4].WangX,etal.Pharmacologicallyblockingp53-dependentapoptosisprotectsintestinalstemcellsandmicefromradiation.SciRep.2015Apr10;5:8566.

MolecularWeight

465.34

Formula

C₂₂H₁₈Cl₂N₈

CASNo.

252917-06-9

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥5.1mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.92%

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