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Medchemexpress/T-5224/HY-12270/5mg
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HY-12270-10mM*1mLinDMSO
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T-5224isaselectiveinhibitorofc-Fos/activatorprotein(AP)-1forrheumatoidarthritistherapy,andinhibitsMMPactivitywithIC50sof10nMforbothMMP-3andMMP-13.

CustomerValidation

  • •CellStemCell.2017May4;20(5):621-634.e6.
  • •CellStemCell.2016Sep1;19(3):326-40.
  • •Endocrinology.2017Nov1;158(11):4064-4075.
  • •JOrthopRes.2017Feb;35(2):311-320.
Description

T-5224isaselectiveinhibitorofc-Fos/activatorprotein(AP)-1forrheumatoidarthritistherapy,andinhibitsMMPactivitywithIC50sof10nMforbothMMP-3andMMP-13.

IC50&Target

IC50:10nM(MMP-3),10nM(MMP-13)

InVitro

T-5224(0-80μM)significantlyinhibitstheinvasion,migration,andMMPactivityofHSC-3-M3cellsinadose-dependentmanner.ThereisnosignificantinfluenceonHSC-3-M3amdOSC-19cellsproliferation[4].

InVivo

G2isobservedinratandmonkeylivermicrosomesasamajormetaboliteofT-5224,suggestingthatG2isnotahuman-specificmetabolite[1].T-5224(300mg/kg,p.o.)inhibitstheproductionofTNF-alphaandotherdownstreameffectorsinC57BL/6mice[2].AdmiNISTrationofT-5224(300mg/kg,p.o.)afterintraperitonealinjectionofLPSimpartesappreciableprotectionagainstacuteelevationsinserumlevelsofTNFα,HMGB1,ALT/ASTaswellasinlivertissuelevelsofMIP-1αandMCP-1,andreducesthelethality(27%)[3].

References

  • [1].UchihashiS,etal.Metabolismofthec-Fos/activatorprotein-1inhibitorT-5224bymultiplehumanUDP-glucuronosyltransferaseisoforms.DrugMetabDispos.2011May;39(5):803-13.

    [2].MiyazakiH,etal.Theeffectsofaselectiveinhibitorofc-Fos/activatorprotein-1onendotoxin-inducedacutekidneyinjuryinmice.BMCNephrol.2012Nov23;13:153.

    [3].IzutaS,etal.T-5224,aselectiveinhibitorofc-Fos/activatorprotein-1,attenuateslipopolysaccharide-inducedliverinjuryinmice.BiotechnolLett.2012Dec;34(12):2175-82.

    [4].KamideD,etal.Selectiveactivatorprotein-1inhibitorT-5224preventslymphnodemetastasisinanoralcancermodel.CancerSci. 2016May;107(5):666-73.

    [5].ZengH,etal.AnIsogenicHumanESCPlatformforFunctionalEvaluationofGenome-wide-Association-Study-IdentifiedDiabetesGenesandDrugDiscovery.CellStemCell.2016Sep1;19(3):326-40.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.9323mL9.6613mL19.3225mL
5mM0.3865mL1.9323mL3.8645mL
10mM0.1932mL0.9661mL1.9323mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[4]

T-5224isdissolvedinDMSOanddilutedinDMEM.

HSC-3-M3cellsarestarvedfor24hwithDMEMcontaining0.5%FBS.Thetopchamberofthecellinvasiondeviceiscoatedwith50μLof0.1×basementmembraneextractsolutionandincubataedovernight.HSC-3-M3cells(5.0×104cells/well)areaddedtothetopchamberwithDMEMcontaining0.5%FBSmixedwith0-80μMT-5224;DMEMwith10%FBSisaddedtothebottomchamberandincubatedfor48h.Thebottomplateisreadusingamultilabelplatereader.Thedataarecomparedwiththestandardcurvetodeterminethefractionofinvadedcells.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2]

T-5224isdissolvedinapolyvinylpyrrolidonesolution,andadjustedtoaconcentrationof30mg/mL.

MiceinLPSgroupareadministeredorallywithpolyvinylpyrrolidonesolutioninthesamevolumeofT-5224solutionimmediatelyafterLPSinjection,whileintheT-5224group,miceareadministeredorallywithT-5224(300mg/kg,p.o.)inthesamemanner.Inthecontrolgroup,micereceivespolyvinylpyrrolidonesolutionorallysoonafterintraperitonealsalineinjection.Bloodsamplesarecollectedforeachmeasurementattheoptimaltime.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].UchihashiS,etal.Metabolismofthec-Fos/activatorprotein-1inhibitorT-5224bymultiplehumanUDP-glucuronosyltransferaseisoforms.DrugMetabDispos.2011May;39(5):803-13.

    [2].MiyazakiH,etal.Theeffectsofaselectiveinhibitorofc-Fos/activatorprotein-1onendotoxin-inducedacutekidneyinjuryinmice.BMCNephrol.2012Nov23;13:153.

    [3].IzutaS,etal.T-5224,aselectiveinhibitorofc-Fos/activatorprotein-1,attenuateslipopolysaccharide-inducedliverinjuryinmice.BiotechnolLett.2012Dec;34(12):2175-82.

    [4].KamideD,etal.Selectiveactivatorprotein-1inhibitorT-5224preventslymphnodemetastasisinanoralcancermodel.CancerSci. 2016May;107(5):666-73.

    [5].ZengH,etal.AnIsogenicHumanESCPlatformforFunctionalEvaluationofGenome-wide-Association-Study-IdentifiedDiabetesGenesandDrugDiscovery.CellStemCell.2016Sep1;19(3):326-40.

MolecularWeight

517.53

Formula

C₂₉H₂₇NO₈

CASNo.

530141-72-1

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥31mg/mL

T5224isdissolvedinpolyvinylpyrrolidoneK60solution[5].

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

References

  • [1].UchihashiS,etal.Metabolismofthec-Fos/activatorprotein-1inhibitorT-5224bymultiplehumanUDP-glucuronosyltransferaseisoforms.DrugMetabDispos.2011May;39(5):803-13.

    [2].MiyazakiH,etal.Theeffectsofaselectiveinhibitorofc-Fos/activatorprotein-1onendotoxin-inducedacutekidneyinjuryinmice.BMCNephrol.2012Nov23;13:153.

    [3].IzutaS,etal.T-5224,aselectiveinhibitorofc-Fos/activatorprotein-1,attenuateslipopolysaccharide-inducedliverinjuryinmice.BiotechnolLett.2012Dec;34(12):2175-82.

    [4].KamideD,etal.Selectiveactivatorprotein-1inhibitorT-5224preventslymphnodemetastasisinanoralcancermodel.CancerSci. 2016May;107(5):666-73.

    [5].ZengH,etal.AnIsogenicHumanESCPlatformforFunctionalEvaluationofGenome-wide-Association-Study-IdentifiedDiabetesGenesandDrugDiscovery.CellStemCell.2016Sep1;19(3):326-40.

Purity:98.41%

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