BiologicalActivity
PotentandselectiveG9a/GLPhistonelysinemethyltransferaseinhibitor(IC50=3.3nM).Exhibits>1000-foldselectivityforG9a/GLPover21othermethyltransferases.Decreaseslevelsoflysine9dimethylationonhistoneH3(H3K9Me2)inPC3cells.
LicensingInformation
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheA366probesummaryontheSGCwebsite.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofA366isreviewedonthechemicalprobeswebsite.
CompoundLibraries
A366isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 329.44 |
| Formula | C19H27N3O2 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1527503-11-2 |
| PubChemID | 76285486 |
| InChIKey | BKCDJTRMYWSXMC-UHFFFAOYSA-N |
| Smiles | COC1=C(OCCCN4CCCC4)C=C(N=C(N)C32CCC3)C2=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| 1eq.HCl | 32.94 | 100 | |
| DMSO | 32.94 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight329.44.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 3.04mL | 15.18mL | 30.35mL |
| 5mM | 0.61mL | 3.04mL | 6.07mL |
| 10mM | 0.3mL | 1.52mL | 3.04mL |
| 50mM | 0.06mL | 0.3mL | 0.61mL |
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