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.Wt | 1002.64 |
| Formula | C49H60ClN9O8S2 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1797406-69-9 |
| PubChemID | 122201421 |
| InChIKey | PTAMRJLIOCHJMQ-PYNGZGNASA-N |
| Smiles | CC1=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
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100.26 | 100 | |
| ethanol | 100.26 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight1002.64.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1mL | 4.99mL | 9.97mL |
| 5mM | 0.2mL | 1mL | 1.99mL |
| 10mM | 0.1mL | 0.5mL | 1mL |
| 50mM | 0.02mL | 0.1mL | 0.2mL |
MolarityCalculator
ReconstitutionCalculator
Thereconstitutioncalculatorallowsyoutoquicklycalculatethevolumeofareagenttoreconstituteyourvial.Simplyenterthemassofreagentandthetargetconcentrationandthecalculatorwilldeterminetherest.