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Medchemexpress/HG-9-91-01(Synonyms: SIK inhibitor 1)/HY-15776/5mg
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Medchemexpress/HG-9-91-01(Synonyms: SIK inhibitor 1)/HY-15776/5mg
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MedChemExpress
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HY-15776-10mM*1mLinDMSO
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HG-9-91-01isapotentandhighlyselectivesalt-inducIBLekinase(SIKs)inhibitorwithIC50sof0.92nM,6.6nMand9.6nMforSIK1,SIK2andSIK3respectively.

CustomerValidation

  • •CellRep.2017Jun13;19(11):2177-2184.
  • •Elife.2015Nov17;4:e08501.
  • •JBiolChem.2015Jul17;290(29):17879-93.
  • •TechnischenUniversitätMünchen.10.03.2017.
Description

HG-9-91-01isapotentandhighlyselectivesalt-induciblekinase(SIKs)inhibitorwithIC50sof0.92nM,6.6nMand9.6nMforSIK1,SIK2andSIK3respectively.

IC50&Target

IC50:0.92/6.6/9.6nM(SIK1/2/3)[1]

InVitro

HG-9-91-01inhibitsanumberofproteintyrosinekinasesthatpossessathreonineresidueatthegatekeepersite,suchasSrcfamilymembers(Src,Lck,andYes),BTK,andtheFGFandEphrinreceptors[1].HG-9-91-01demonstratesastrongcorrelationbetweenthepotencyofSIK2inhibitionandenhancedIL-10production.Inagreementwiththesereports,pretreatingBMDCswithHG-9-91-01,arecentlydescribedinhibitorofSIK1-3,alongwithseveralotherkinases,resultsinconcentration-dependentpotentiationofzymosan-inducedIL-10productionwithanEC50~200nMandamaximumeffectsimilartothatobservedwithPGE2[2].HG-9-91-01hasmorethana100-foldgreaterpotencyagainstSIKsthanAMPK(IC50=4.5μM)inacell-freeassay.HG-9-91-01treatmentdosedependentlyincreasedmRNAexpressionofPck1andG6pcandthateffectissimilarincellstreatedwith4μMHG-9-91-01or0.1μMglucagon.Consistentwiththisobservation,thereisalsoadose-dependentincreaseinglucoseproductionfollowingHG-9-91-01treatment[3].

References

  • [1].ClarkK,etal.PhosphorylationofCRTC3bythesalt-induciblekinasescontrolstheinterconversionofclassicallyactivatedandregulatorymacrophages.ProcNatlAcadSciUSA.2012Oct16;109(42):16986-91.

    [2].SundbergTB,etal.Small-moleculescreeningidentifiesinhibitionofsalt-induciblekinasesasatherapeuticstrategytoenhanceimmunoregulatoryfunctionsofdendriticcells.ProcNatlAcadSciUSA.2014Aug26;111(34):12468-73.

    [3].PatelK,etal.TheLKB1-salt-induciblekinasepathwayfunctionsasakeygluconeogenicsuppressorintheliver.NatCommun.2014Aug4;5:4535.

    [4].MujahidN,etal.AUV-IndependentTopicalSmall-MoleculeApproachforMelaninProductioninHumanSkin.CellRep.2017Jun13;19(11):2177-2184.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.7616mL8.8078mL17.6156mL
5mM0.3523mL1.7616mL3.5231mL
10mM0.1762mL0.8808mL1.7616mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

HG-9-91-01isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse[2].

BonemarrowisharvestedfromfemursandtibiasofC57BL/6mice.Bone-marrow-deriveddendriticcells(BMDCs)aredifferentiatedDMEMsupplementedwith2mMGlutaMAX,10%(vol/vol)FBS,Penicillin,Streptomycin,and2%mousegranulocyte-macrophagecolony-stimulatingfactor(GM-CSF)-conditionedmediaderivedfrommurineLcells.Culturesaredifferentiatedfor7dandroutinelyanalyzedfor>90%CD11c(allophycocyanin(APC)anti-CD11ccloneHL3)positivitybyflowcytometrybeforeuseinexperiments.Lentiviraltransductionofbonemarrowculturesisconductedbyadditionof293TculturesupernatantscontaininglentiviralparticlesencodingtheCREB-dependentluciferasereporterconstructorCRTC3targetingorcontrolshRNAs1dpostisolation.StableintegrationoflentiviralshRNAconstructsisselectedbyadditionofpuromycin(3μg/mL)onday4posttransduction.After2d,stablytransducedBMDCsarereleasedfromselectionandusedinsubsequentassays.Unlessotherwiseindicated,cellsaretreatedfor2dwithPGE2(5μM)orHG-9-91-01(0.5μM)oranequivalentconcentrationofDMSO(≤0.5%)andthenstimulatedfor18hwithLPS(100ng/mL),R848(10μg/mL),orZymosan(4μg/mL)[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].ClarkK,etal.PhosphorylationofCRTC3bythesalt-induciblekinasescontrolstheinterconversionofclassicallyactivatedandregulatorymacrophages.ProcNatlAcadSciUSA.2012Oct16;109(42):16986-91.

    [2].SundbergTB,etal.Small-moleculescreeningidentifiesinhibitionofsalt-induciblekinasesasatherapeuticstrategytoenhanceimmunoregulatoryfunctionsofdendriticcells.ProcNatlAcadSciUSA.2014Aug26;111(34):12468-73.

    [3].PatelK,etal.TheLKB1-salt-induciblekinasepathwayfunctionsasakeygluconeogenicsuppressorintheliver.NatCommun.2014Aug4;5:4535.

    [4].MujahidN,etal.AUV-IndependentTopicalSmall-MoleculeApproachforMelaninProductioninHumanSkin.CellRep.2017Jun13;19(11):2177-2184.

MolecularWeight

567.68

Formula

C₃₂H₃₇N₇O₃

CASNo.

1456858-58-4

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

HG9-91-01isdissolvedin30%propyleneglycolplus70%ethanol[4].

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

References

  • [1].ClarkK,etal.PhosphorylationofCRTC3bythesalt-induciblekinasescontrolstheinterconversionofclassicallyactivatedandregulatorymacrophages.ProcNatlAcadSciUSA.2012Oct16;109(42):16986-91.

    [2].SundbergTB,etal.Small-moleculescreeningidentifiesinhibitionofsalt-induciblekinasesasatherapeuticstrategytoenhanceimmunoregulatoryfunctionsofdendriticcells.ProcNatlAcadSciUSA.2014Aug26;111(34):12468-73.

    [3].PatelK,etal.TheLKB1-salt-induciblekinasepathwayfunctionsasakeygluconeogenicsuppressorintheliver.NatCommun.2014Aug4;5:4535.

    [4].MujahidN,etal.AUV-IndependentTopicalSmall-MoleculeApproachforMelaninProductioninHumanSkin.CellRep.2017Jun13;19(11):2177-2184.

Purity:95.83%

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