BiologicalActivity
PotentBETbromodomaininhibitor;exhibitsinhibitoryactivityatbromodomain-containingprotein(BRD)2andBRD4(IC50valuesare98and220nMrespectively).InducesapoptosisandG1cellcyclearrestinBETinhibitor-sensitivecelllines(MV4;11).AlsodownregulatesAuroraBexpressioninMV4;11cells.Cellpermeable.
LicensingInformation
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisitthePFI1probesummaryontheSGCwebsite.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofPFI1isreviewedonthechemicalprobeswebsite.
CompoundLibraries
PFI1isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 347.39 |
| Formula | C16H17N3O4S |
| Storage | StoreatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 1403764-72-6 |
| PubChemID | 71271629 |
| InChIKey | TXZPMHLMPKIUGK-UHFFFAOYSA-N |
| Smiles | O=C2NC1=CC=C(NS(C3=CC=CC=C3OC)(=O)=O)C=C1CN2C |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 17.37 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight347.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.88mL | 14.39mL | 28.79mL |
| 5mM | 0.58mL | 2.88mL | 5.76mL |
| 10mM | 0.29mL | 1.44mL | 2.88mL |
| 50mM | 0.06mL | 0.29mL | 0.58mL |
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ProductDatasheets
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