BiologicalActivity
PotentandselectiveSAM-competitiveEZH2inhibitor(IC50=4mM).Exhibits>60foldselectivityforEZH2overEZH1andarangeofothermethyltransferases.Inhibitsproliferationofprostatecancercelllinesinvitro.
LicensingInformation
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheGSK343probesummaryontheSGCwebsite.
TechnicalData
M.Wt | 541.69 |
Formula | C31H39N7O2 |
Storage | Storeat-20°C |
Purity | ≥98%(HPLC) |
CASNumber | 1346704-33-3 |
PubChemID | 71268957 |
InChIKey | ULNXAWLQFZMIHX-UHFFFAOYSA-N |
Smiles | CCCC1=C(C(NC(C)=C1)=O)CNC(C2=C3C=NN(C3=CC(C4=CC=NC(N5CCN(CC5)C)=C4)=C2)C(C)C)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 10.83 | 20mMwithgentlewarming |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight541.69.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 1.85mL | 9.23mL | 18.46mL |
5mM | 0.37mL | 1.85mL | 3.69mL |
10mM | 0.18mL | 0.92mL | 1.85mL |
50mM | 0.04mL | 0.18mL | 0.37mL |
MolarityCalculator
ReconstitutionCalculator
Thereconstitutioncalculatorallowsyoutoquicklycalculatethevolumeofareagenttoreconstituteyourvial.Simplyenterthemassofreagentandthetargetconcentrationandthecalculatorwilldeterminetherest.