Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGNE-371Cat.No.:HY-112803CASNo.:1926986-36-8分?式:C??H??N?O?分?量:431.49作?靶點(diǎn):DNA/RNASynthesis作?通路:CellCycle/DNADamage儲(chǔ)存?式:4°C,protectfromlight,storedunderargon*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedunderargon)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(115.88mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3176mL11.5878mL23.1755mL5mM0.4635mL2.3176mL4.6351mL10mM0.2318mL1.1588mL2.3176mL請根據(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(protectfromlight,storedunderargon)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.5mg/mL(5.79mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.79mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.79mM);ClearsolutionBIOLOGICALACTIVITY?物活性GNE-371?種針對?類轉(zhuǎn)錄起始因?TFIID亞1和類轉(zhuǎn)錄起始因?TFIID亞1的第?溴端結(jié)構(gòu)域的?效選擇性化學(xué)探針，對TAF1(2)的IC50值為10nM。IC50&TargetIC50:10nM(TAF1(2))[1].體外研究GNE-371(compound27)bindsTAF1(2)withanIC50of10nMwhilemaintainingexcellentselectivityoverotherbromodomain-familymembers.GNE-371isalsoactiveinacellular-TAF1(2)target-engagementassay(IC50=38nM)andexhibitsanti-proliferativesynergywiththeBETinhibitorJQ1,suggestingengagementofendogenousTAF1byGNE-371andfurthersupportingtheuseofGNE-371inmechanisticandtarget-validationstudies[1].REFERENCES[1].WangS,etal.GNE-371,aPotentandSelectiveChemicalProbefortheSecondBromodomainsofHumanTranscription-Initiation-FactorTFIIDSubunit1andTranscription-Initiation-FactorTFIIDSubunit1-like.JMedChem.2018Oct25;61(20):9301-9315.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly