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主营:分子类,蛋白类,抗体类,生化类试剂
℡ 4000-520-616
℡ 4000-520-616
Tocris/MZ 1/6154/5/5 mg
产品编号:6154
市  场 价:¥6700.00
场      地:美国(厂家直采)
产品分类: 分子类>核酸酶类>连接酶>
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:$335.00
品      牌: Tocris
公      司:Tocris Bioscience
公司分类:
Tocris/MZ 1/6154/5/5 mg
商品介绍
Description:(+)-JQ1basedPROTACthatselectivelydegradesBRD4incells
ChemicalName:(2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity:≥98%(HPLC)
BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferences

BiologicalActivity

CellpenetrantProteolysisTargetingChimera(PROTAC)compoundbasedon(+)-JQ1(Cat.No.4499)conjugatedtoavonHippel-Lindau(VHL)ligand.RetainshighaffinityforBRD2,BRD3andBRD4bromodomains(Kd=13-60nM)butinducespreferentialdegradationofBRD4overBRD2andBRD3(DC50valuesfordegradationofBRD4are8and23nMinH661andH838cells,respectively).ExhibitspotentcytotoxicityandantiproliferativeeffectsinAMLcelllines(pEC50=7.6inMv4;11cells).NegativecontrolcisMZ1alsoavailable.

PROTACsarebi-functionalsmallmoleculesthatharnesstheubiquitin/proteasomesystem(UPS)toselectivelyandcatalyticallyremovetargetproteinsfromcells.

LicensingInformation

SoldunderlicencefromtheUniversityofDundee

ExternalPortalInformation

Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofMZ1isreviewedontheChemicalProbeswebsite.

TechnicalData

M.Wt1002.64
FormulaC49H60ClN9O8S2
StorageStoreat-20°C
Purity≥98%(HPLC)
CASNumber1797406-69-9
PubChemID122201421
InChIKeyPTAMRJLIOCHJMQ-PYNGZGNASA-N
SmilesCC1=C(C2=C(N3C(C)=NN=C3[C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)O)=O)=O)=O)S1)C

Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.

AllTocrisproductsareintendedforlaboratoryresearchuseonly.

SolubilityData

SolventMaxConc.mg/mLMaxConc.mM
Solubility
DMSO100.26100
ethanol100.26100

PreparingStockSolutions

Thefollowingdataisbasedontheproductmolecularweight1002.64.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.

Concentration/SolventVolume/Mass1mg5mg10mg
1mM1mL4.99mL9.97mL
5mM0.2mL1mL1.99mL
10mM0.1mL0.5mL1mL
50mM0.02mL0.1mL0.2mL