GNE-371-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGNE-371Cat.No.:HY-112803CASNo.:1926986-36-8分⼦式:C₂₄H₂₅N₅O₃分⼦量:431.49作⽤靶点:DNA/RNASynthesis作⽤通路:CellCycle/DNADamage储存⽅式:4°C,protectfromlight,storedunderargon*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedunderargon)溶解性数据体外实验DMSO:50mg/mL(115.88mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3176mL11.5878mL23.1755mL5mM0.4635mL2.3176mL4.6351mL10mM0.2318mL1.1588mL2.3176mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight,storedunderargon)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.5mg/mL(5.79mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.79mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.79mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GNE-371⼀种针对⼈类转录起始因⼦TFIID亚1和类转录起始因⼦TFIID亚1的第⼆溴端结构域的⾼效选择性化学探针，对TAF1(2)的IC50值为10nM。IC50&TargetIC50:10nM(TAF1(2))[1].体外研究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