BiologicalActivity
PotentandselectivePRMT5inhibitor(IC50=4nM).SelectiveforPRMT5overapanelofotherPRMTsandlysinemethyltransferases.Inhibitsproliferationofmantlecelllymphoma(MCL)invitro.
LicensingInformation
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheGSK591probesummaryontheSGCwebsite.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofGSK591isreviewedontheChemicalProbeswebsite.
TechnicalData
| M.Wt | 453.41 |
| Formula | C22H28N4O2.2HCl |
| Storage | DesiccateatRT |
| Purity | ≥97%(HPLC) |
| CASNumber | 1616391-87-7 |
| PubChemID | 124201849 |
| InChIKey | CDKUMVXFXBTOBE-FJSYBICCSA-N |
| Smiles | O[C@@H](CNC(C1=CC=NC(NC2CCC2)=C1)=O)CN3CC4=CC=CC=C4CC3.Cl.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| water | 45.34 | 100 | |
| DMSO | 45.34 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight453.41.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.21mL | 11.03mL | 22.06mL |
| 5mM | 0.44mL | 2.21mL | 4.41mL |
| 10mM | 0.22mL | 1.1mL | 2.21mL |
| 50mM | 0.04mL | 0.22mL | 0.44mL |
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