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Product Name | P005091 |
Description | Purity >98%. 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 (EC50 s = 4.2 and 4.3 µM, respectively) with little activity against other classes of proteases, including caspases, cathepsins, calpain, metalloproteases, and serine proteases (EC50 s = > 100 µM). P005091 has been shown to accelerate the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 = 11 µM) and to inhibit the growth of HCT116 human colorectal cancer cells (EC50 = 11 µM) synergistically with doxorubicin, etoposide, or mechlorethamine. In vivo, 10 mg/kg P005091 prolongs survival and reduces tumor growth in mice bearing human multiple myeloma and B cell leukemia xenografts. |
Size | n/a |
Concentration | n/a |
Applications | n/a |
Other Names | 1-[5-[(2,3-dichlorophenyl)thio]-4-nitro-2-thienyl]-ethanone, P5091 |
Gene, Accession, CAS # | CAS: 882257-11-6 |
Catalog # | LS-H9236 |
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Order / More Info | P005091 from LIFESPAN BIOSCIENCES INC. |
Product Specific References | n/a |
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