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Medchemexpress/EMD638683/HY-15193/10mg

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MedChemExpress

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HY-15193-10mM*1mLinDMSO

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4000-520-616

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EMD638683isahighlyselectiveSGK1inhibitorwithIC₅₀of3μM.

CustomerValidation

•JAutoimmun.2016Feb;67:90-101.
•JBoneMinerRes.2015Nov;30(11):1959-68.
•FASEBJ.2015Sep;29(9):3737-49.
•EnvironToxicolPharmacol.2014Sep;38(2):374-8.
•ActaBiochimBiophysSin(Shanghai).2017Apr1;49(4):302-310.

Description	EMD638683isahighlyselectiveSGK1inhibitorwithIC₅₀of3μM.
IC₅₀&Target	IC50:3μM(SGK1)^[1]
InVitro	EMD638683isaSGK1inhibitor.EMD638683inhibitstheNDRG1(N-Mycdownstream-regulatedgene1)phosphorylation,aneffectrequiring3.35±0.32μMEMD638683inthecellculturemediumforhalfmaximaleffect(IC₅₀).EMD638683hasalsoaninhibitoryeffectoncAMP-dependentproteinkinase(PKA),mitogen-andstress-activatedproteinkinase1(MSK1),proteinkinaseC-relatedkinase2(PKR2),andtheSGKisoformsSGK2andSGK3^[1].Inboth,controlandEMD638683(50µM)-treatedCaCo-2cells,rADIationsignificantlyincreasesthepercentageofCaCo-2cellsundergoinglateapoptosis.EMD638683treatmentalonetendstoenhancethepercentageofapoptoticCaCo-2cells.FollowingradiationthepercentageofapoptoticEMD638683-treatedCaCo-2cellsissignificantlyhigherthanthepercentageofapoptoticcontrolcells.Thus,EMD638683treatmentsignificantlyaugmentstheapoptosisfollowingradiation^[2].
InVivo	ThecolonissignificantlylongerandthecolonweightsignificantlylowerinEMD638683-treatedmicethaninplacebo-treatedmice,afindingpointingtoaninfluenceofEMD638683ontumorgrowthfollowingchemicalcarcinogenesis.Inaddition,thestomachweightissignificantlylowerintheEMDtreatedgroup.Mostimportantly,thenumberofdevelopingtumorsfollowingcarcinogenictreatmentissignificantlybluntedbyEMD638683treatment^[2].EMD638683(20mg/kg,intragastrically)preventsprogressionofmonocrotaline(MCT)-inducedpulmonaryvascularremodelinginrats.HemodynamiccharacteristicsshowthatEMD638683treatmentattenuatesrightventricularsystolicpressure(RVSP)(15.8±2.5vs.28.2±3.1mmHg;P<0.05; n="6)" and="" right="" ventricular="" hypertrophy="" index="" (rvhi)="" (0.27±0.02="" vs.=""><0.05; n="6)" compare="" to="" vehicle-dosed="">^[3].
References	[1].AckermannTF,etal.EMD638683,anovelSGKinhibitorwithantihypertensivepotency.CellPhysiolBiochem.2011;28(1):137-46. [2].TowhidST,etal.InhibitionofcolonictumorgrowthbytheselectiveSGKinhibitorEMD638683.CellPhysiolBiochem.2013;32(4):838-48. [3].XiX,etal.Serum-glucocorticoidregulatedkinase1regulatesmacrophagerecruitmentandactivationcontributingtomonocrotaline-inducedpulmonaryarterialhypertension.CardiovascToxicol.2014Dec;14(4):368-78. [4].ZhouH,etal.Inhibitionofserum-andglucocorticoid-inducIBLekinase1enhancesTLR-mediatedinflammationandpromotesendotoxin-drivenorganfailure.FASEBJ.2015Sep;29(9):3737-49.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.7447mL	13.7234mL	27.4469mL
5mM	0.5489mL	2.7447mL	5.4894mL
10mM	0.2745mL	1.3723mL	2.7447mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

CellAssay
^[2]

EMD638683isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse^[2].

Coloncarcinoma(CaCo-2)cellsaregrownincompleteDMEMmediumcontaining10%fetalcalfserum,1%sodiumpyruvate,1%penicillin-streptomycinand1%non-essentialaminoacidsunderstandardcultureconditions(37°C,5%CO₂).10⁵cellsareseededin6wellplatesandculturedwithfreshculturemediumfor24h,afterwhichEMD638683(50µM)isappliedfor24hours.Forcomparison,thecellsaretreatedwiththesolvent(0.2μLDMSO)andonesolventcontrolisanalysedwitheachsetofexperiments.Thecellsaresubsequentlyexposedto3.18minradiation(3Gray).Afterfurtherincubationfor72hinthepresenceorabsenceofEMD638683(50µM)thecellsareanalyzedutilizingflowcytometry^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
^[3]

EMD638683issynthesizedbyHaoyuan(Shanghai,China)anddissolvedin1%DMSO^[3].

RatandMice^[3]
PAHisinducedin2-month-oldmaleSprague-DawleyratsbyadministeringasinglesubcutaneousinjectionofMCT(60mg/kg,n=12).Ratsinthecontrolgrouparegiventhevehiclesaline(0.5mL,subcutaneously,n=12).SixratsineachgrouparegivenEMD638683(20mg/kg)intragastricallyoncedailystarting2dayspriortoMCTtreatment.Ratsareanesthetizedwithsodiumpentobarbital(50mg/kgintraperitoneally).Rightventricularsystolicpressure(RVSP),rightventricularhypertrophy,andpulmonaryvascularremodelingareevaluated21daysafterMCTinjection.Attheageof10-12weeks,maleSGK1^-/-miceandtheirwild-type(WT)littermatesaregivenMCTindosesof60mg/100gbodyweightonceaweekfor8consecutiveweeksbysubcutaneousinjectiontoinducePAH.Thereareeightmicepergroup.Miceareanesthetizedwithsodiumpentobarbital(50mg/kgintraperitoneally)onday8afterthelastMCTadministration.ThenRVSP,rightventricularhypertrophy,andpulmonaryvascularremodelingareevaluated.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].AckermannTF,etal.EMD638683,anovelSGKinhibitorwithantihypertensivepotency.CellPhysiolBiochem.2011;28(1):137-46.
[2].TowhidST,etal.InhibitionofcolonictumorgrowthbytheselectiveSGKinhibitorEMD638683.CellPhysiolBiochem.2013;32(4):838-48.
[3].XiX,etal.Serum-glucocorticoidregulatedkinase1regulatesmacrophagerecruitmentandactivationcontributingtomonocrotaline-inducedpulmonaryarterialhypertension.CardiovascToxicol.2014Dec;14(4):368-78.
[4].ZhouH,etal.Inhibitionofserum-andglucocorticoid-induciblekinase1enhancesTLR-mediatedinflammationandpromotesendotoxin-drivenorganfailure.FASEBJ.2015Sep;29(9):3737-49.

MolecularWeight

364.34

Formula

C₁₈H₁₈F₂N₂O₄

CASNo.

1181770-72-8

Storage

Powder	-20°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO

EMD638683isfixedin4%formaldehyde^[4].

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

References

[1].AckermannTF,etal.EMD638683,anovelSGKinhibitorwithantihypertensivepotency.CellPhysiolBiochem.2011;28(1):137-46.
[2].TowhidST,etal.InhibitionofcolonictumorgrowthbytheselectiveSGKinhibitorEMD638683.CellPhysiolBiochem.2013;32(4):838-48.
[3].XiX,etal.Serum-glucocorticoidregulatedkinase1regulatesmacrophagerecruitmentandactivationcontributingtomonocrotaline-inducedpulmonaryarterialhypertension.CardiovascToxicol.2014Dec;14(4):368-78.
[4].ZhouH,etal.Inhibitionofserum-andglucocorticoid-induciblekinase1enhancesTLR-mediatedinflammationandpromotesendotoxin-drivenorganfailure.FASEBJ.2015Sep;29(9):3737-49.

Purity:99.74%

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