MolecularWeight: | 348.22 |
Formula: | C12H7Cl2NO3S2 |
Purity: | ≥98% |
CAS#: | 882257-11-6 |
Solubility: | DMSOupto100mM |
ChemicalName: | 1-(5-((2,3-dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethanone |
Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:
P5091(P005091)isanovelpotentandselectiveinhibitorofubiquitin-specificprotease7(USP7)withanIC50~4.2μM.ItdoesnotinhibitotherDUBsorotherfamiliesofcysteineproteasestested(EC50>100mM).ItinducesapoptosisinMMcellsresistanttoconventionalandbortezomibtherapies.BiochemicalandgeneticstudiesshowedthatblockadeofHDM2andp21abrogatedP5091-inducedcytotoxicity.Inanimaltumormodelstudies,P5091waswelltolerated,anditinhibitedtumorgrowth,andprolongssurvival.CombiningP5091withlenalidomide,HDACinhibitorSAHA,ordexamethasonetriggeredsynergisticanti-MMactivity.
HowtoUse:
- Invitro:P5091wasusedat5-12.5µMfinalconcentrationinvariousinvitroassays.
- Invivo:P5091wasadmiNISTeredthroughIVinjectionat10mg/kgtwiceweeklyfor3weeks.
Reference:
- 1.ChauhanD,etal.Asmallmoleculeinhibitorofubiquitin-specificprotease-7inducesapoptosisinmultiplemyelomacellsandovercomesbortezomibresistance.(2012)CancerCell.22(3):345-58.
- P5091_spec.pdf
- P5091_MSDS.pdf
Productsareforresearchuseonly.Notforhumanuse.