GSK2807-Trifluoroacetate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK2807TrifluoroacetateCat.No.:HY-104009ACASNo.:2245255-66-5分?式:C??H??F?N?O?分?量:566.53作?靶點(diǎn):HistoneMethyltransferase作?通路:Epigenetics儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥250mg/mL(441.28mM)H2O:≥50mg/mL(88.26mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7651mL8.8257mL17.6513mL5mM0.3530mL1.7651mL3.5303mL10mM0.1765mL0.8826mL1.7651mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.67mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.67mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.67mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:100mg/mL(176.51mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性GSK2807TrifluoroacetateSMYD3有效的、有選擇性的，SAM競(jìng)爭(zhēng)性抑制劑，其Ki值為14nM，IC50為130nM。IC50&TargetSMYD3SMYD314nM(Ki)130nM(IC50)體外研究Ahigh-resolutioncrystalstructurerevealsthatGSK2807bridgesthegapbetweentheSAM-bindingpocketandthesubstratelysinetunnelofSMYD3.GSK2807is24-foldselectiveforSMYD3incomparisonwiththecloselyrelatedenzymeSMYD2(Ki=14±6nMand345±36nM,respectively)[1].REFERENCES[1].VanAllerGS,etal.Structure-BasedDesignofaNovelSMYD3InhibitorthatBridgestheSAM-andMEKK2-BindingPockets.Structure.2016May3;24(5):774-781.[2].KaniskanHü,etal.InhibitorsofProteinMethyltransferasesandDemethylases.ChemRev.2018Feb14;118(3):989-1068.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl