P005091

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 1-[5-[(2,3-dichlorophenyl)thio]-4-nitro-2-thienyl]-ethanone
• Correlated keywords
  • ubiquitin-specific ubiquitins specifics proteases USPs UBPs ubiquitylation proteasome USP7 cysteines USP-7 7 seven prostate cancers deubiquitylation HDM2 HDMs HDM-2 2 two E3 ligase tumors suppressors p53 anticancer anti-cancer anti multiple myeloma bortezomib therapy therapies deubiquintinase DUB selective USP/UBP P-005091 Ps 005091 P-5091 P5091 5091 trisubtituted thiophene inhibits inhibitions inhibitors caspases cathepsins calpain metalloproteases serines myeloma doxorubicin etoposide mechlorethamine in vivos B B-cells Bcells leukemia growths intracellular signaling P5091 HCT-116
• Product Overview:
  Ubiquitin-specific proteases (USP/UBP) remove ubiquitin from proteins, sparing them from degradation by the proteasome. USP7 is a cysteine protease associated with prostate cancer that selectively deubiquitylates HDM2, the ubiquitin E3 ligase for the tumor suppressor p53. P005091 is a trisubstituted thiophene that inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 ?M, respectively) with little activity against other classes of proteases, including caspases, cathepsins, calpain, metalloproteases, and serine proteases (EC50s = > 100 ?M).{24461,24462} P005091 has been shown to accelerate the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 = 11 ?M) and to inhibit the growth of HCT116 human colorectal cancer cells (EC50 = 11 ?M) synergistically with doxorubicin, etoposide, or mechlorethamine.{24461} In vivo, 10 mg/kg P005091 prolongs survival and reduces tumor growth in mice bearing human multiple myeloma and B cell leukemia xenografts.{24461}