GSK620-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK620Cat.No.:HY-137892CASNo.:2088410-46-0分?式:C??H??N?O?分?量:325.36作?靶點(diǎn):EpigeneticReaderDomain作?通路:Epigenetics儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:62.5mg/mL(192.09mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0735mL15.3676mL30.7352mL5mM0.6147mL3.0735mL6.1470mL10mM0.3074mL1.5368mL3.0735mL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。-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(6.39mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.39mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK620?種有效的?服活性泛BD2抑制劑，具有良好的?譜選擇性、可開發(fā)性和體內(nèi)?服藥代動(dòng)?學(xué)，對(duì)BET-BD2家族蛋?具有?度選擇性，其選擇性超過所有其他BETbromodomains200倍以上。GSK620在?全?中表現(xiàn)出抗炎表型。體外研究GSK620showsananti-inflammatoryphenotypeinhumanwholeblood.HumanbloodsamplesarestimulatedwithLPS,whichproducesastrongimmuneresponse.Themonocytechemattractantprotein1(MCP-1/CCL2)ismeasured.Thisisachemokinewhichrecruitsmonocytes,memoryTcells,anddendriticcellstositesofinflammation.GSK620reducestheMCP-1responseinaconcentration-dependentmannerwith(anexpected)-1logdropoffinpotencyrelativetothebiochemicalBRD4BD2potenciesobserved[1].體內(nèi)研究HighlightingtheutilityofGSK620asaninvivotool,efficacyisobservedinseparatemodelsofinflammatoryarthritis,psoriasis,andhepatitis[1].REFERENCES[1].SealJT,etal.TheOptimizationofaNovel,WeakBromoandExtraTerminalDomain(BET)BromodomainFragmentLigandtoaPotentandSelectiveSecondBromodomain(BD2)Inhibitor.JMedChem.2020;63(17):9093-9126.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.