Description:PotentandselectiveDNA-PKinhibitorAlternativeNames:KU57788ChemicalName:8-(4-Dibenzothienyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-onePurity:≥99%(HPLC)BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferencesBiologicalActivityPotentandselectiveDNA-PKinhibitor(IC50=14nM).SelectiveforDNA-PKoverarangeofkinasesincludingmTOR,PI3-K,ATMandATR.Potentiatestheeffectsofdoxorubicin(Cat.No.2252)andetoposide(Cat.No.1226)invitroandetoposideinvivo.AlsoenhancesCRISPR-Cas9-mediatedhomology-directedrepair(HDR)efficiency2to3-fold,anddecreasesnonhomologousend-joining(NHEJ)frequency~40%.TechnicalDataM.Wt413.49FormulaC25H19NO3SStorageStoreat+4°CPurity≥99%(HPLC)CASNumber503468-95-9PubChemID11327430InChIKeyJAMULYFATHSZJM-UHFFFAOYSA-NSmilesO=C1C3=C(C(C4=CC=CC5=C4SC6=C5C=CC=C6)=CC=C3)OC(N2CCOCC2)=C1Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.AllTocrisproductsareintendedforlaboratoryresearchuseonly.SolubilityDataSolventMaxConc.mg/mLMaxConc.mMSolubilityDMSO2.075mMwithgentlewarmingPreparingStockSolutionsThefollowingdataisbasedontheproductmolecularweight413.49.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.Concentration/SolventVolume/Mass1mg5mg10mg1mM2.42mL12.09mL24.18mL5mM0.48mL2.42mL4.84mL10mM0.24mL1.21mL2.42mL50mM0.05mL0.24mL0.48mLMolarityCalculatorMolarityCalculatorCalculatethemass,volume,orconcentrationrequiredforasolution.ReconstitutionCalculatorReconstitutionCalculatorDilutionCalculatorDilutionCalculatorCalculatethedilutionrequiredtoprepareastocksolution.ProductDatasheetsCertificateofAnalysis/ProductDatasheetSafetyDatasheetSelectanotherlanguage:EnglishGermanFrenchSpanishViewSDSReferencesReferencesarepublicationsthatsupporttheproducts'biologicalactivity.Zhaoetal(2006)PreclinicalevaluationofapotentnovelDNA-dependentproteinkinaseinhibitorNU7441.CancerRes.665354PMID:16707462Willmoreetal(2008)DNA-dependentproteinkinaseisatherapeutictargetandanindicatorofpoorprognosisinB-cellchroniclymphocyticleukemia.Clin.CancerRes.143984PMID:18559621Leahyetal(2004)IdentificationofahighlypotentandselectiveDNA-dependentproteinkinase(DNA-PK)inhibitor(NU7441)byscreeningofchromenonelibraries.Bioorg.Med.Chem.Lett.146083PMID:15546735Robertetal(2015)PharmacologicalinhibitionofDNA-PKstimulatesCas9-mediatedgenomeediting.GenomeMed.793PMID:26307031Keywords:NU7441,supplier,potent,selective,DNA-dependent,protein,kinases,inhibitors,inhibits,Checkpoint,Control,Kinases,DNA-PK,NU7441,KU57788,CRISPR,Cas9,HDR,NHEJ,homology,directed,repair,nonhomologous,end,joining,KU,57788,DNA-dependent,Protein,Kinase,Checkpoint,Control,Kinases,CRISPR,Reagents,DNA-dependent,Protein,Kinase,TocrisBioscience
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌,其产品也广为各大药厂、大学、研究机构,超过五万名科学研究者所采用。 目前,產品內容已超過一千六百種以上,並每年持續不斷的增加新的產品。目前,产品内容已超过一千六百种以上,并每年持续不断的增加新的产品。
Tocris bioscience是位于英国布里斯托尔(Bristol)的高品质试剂提供商,共有2000多种产品,主要集中在神经科学和信号传导领域,产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等,主要产品包括GPCR ligands,神经传递素,离子通道调控剂,信号通路抑制剂等,这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者,其生产的影响神经系统的化学物质被多次引用,这些物质很多都来自Jeff Watkins(Tocris 的创立人)在Bristol大学原创性的研究工作。
Tocris Bioscience的主要产品包括:
Small Molecules
Peptides
Aptamers
Controlled Substances
Compound Libraries
DREADD Ligands
Fluorescent Imaging
Ligand Sets
Optopharmacology
Reagents
Toxins
按照研究领域细分:
Cancer
Cardiovascular System
Endocrinology
Immunology
Neuroscience
Pain & Inflammation
Respiratory System