GeA-69-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGeA-69Cat.No.:HY-108708CASNo.:2143475-98-1分?式:C??H??N?O分?量:300.35作?靶點(diǎn):PARP作?通路:CellCycle/DNADamage;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:≥125mg/mL(416.18mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.3294mL16.6472mL33.2945mL5mM0.6659mL3.3294mL6.6589mL10mM0.3329mL1.6647mL3.3294mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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(6.93mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(6.93mM);ClearsolutionBIOLOGICALACTIVITY?物活性GeA-69?種選擇性的PARP14變構(gòu)抑制劑，靶向作?于macrodomain2(MD2)，Kd值為2.1μM。GeA-69參與DNA損傷修復(fù)機(jī)制，能夠防?PARP14MD2募集到激光誘導(dǎo)的DNA損傷部位。IC50&TargetPARP142.1μM(Kd)體外研究GeA-69(compound1)(50μMand250μM;pre-damagefor1hor0.5,1,2.5min)engagesPARP14MD2inintactcellsandpreventsitslocalisationtositesofDNAdamageinU-2OScells[2].GeA-69(25nM-250μM;72h)exhibitsmoderatecytotoxicityamongHeLa,U-2OSandHEK293cellsandhighlycellpermeablewith2%passingparacellularand98%transcellularoverthemembrane[2].CellCytotoxicityAssay[2]CellLine:HeLa,U-2OSandHEK293cellsConcentration:25nM-250μMIncubationTime:72hoursResult:ResultedmoderatecytotoxicityagainstnormalcellswithEC50_HeLa=58μM,EC50_U-2OS=52μM,EC50_HEK293=54μM.REFERENCES[1].MoustakimM,etal.Discoveryofanovelallostericinhibitorscaffoldforpolyadenosine-diphosphate-ribosepolymerase14(PARP14)macrodomain2.BioorgMedChem.2018Jul15;26(11):2965-2972.[2].SchullerM,etal.DiscoveryofaSelectiveAllostericInhibitorTargetingMacrodomain2ofPolyadenosine-Diphosphate-RibosePolymerase14.ACSChemBiol.2017Nov17;12(11):2866-2874.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresea