BiologicalActivity
InhibitorofBmi1/Ring1A,subunitsofthepolycombrepressivecomplex1(PRC1);inhibitsself-ubiquitination(IC50=3.9μM)butdoesnotincreasecellularlevelsofeithersubunit.PreventsBmi1/Ring1A-mediatedubiquitinationanddrug-induceddegradationoftopoisomerase2α(Top2α).AlsoshowntoinhibittheinvitroE3ubiquitinligaseactivityofRNF2andaBmi1/RNF2complex,inhibitingH2A/H2AXubiquitination.Blockspolycombrepressorcomplex(PRC)1-mediatedhistoneH2Aubiquitinationinvitroandinvivo.
CompoundLibraries
PRT4165isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 235.24 |
| Formula | C15H9NO2 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 31083-55-3 |
| PubChemID | 207893 |
| InChIKey | OMHZFEWYVFWVLI-UHFFFAOYSA-N |
| Smiles | O=C(C2=CC=CC=C2C3=O)/C3=CC1=CC=CN=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| 1eq.HCl | 1.18 | 5mMwithgentlewarming | |
| DMSO | 23.52 | 100 | |
| ethanol | 2.35 | 10mMwithgentlewarming |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight235.24.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 4.25mL | 21.25mL | 42.51mL |
| 5mM | 0.85mL | 4.25mL | 8.5mL |
| 10mM | 0.43mL | 2.13mL | 4.25mL |
| 50mM | 0.09mL | 0.43mL | 0.85mL |
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