A trisubstituted thiophene that selectively inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 μM

P005091 – 10 mg

Brand:
Cayman
CAS:
882257-11-6
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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 μM, respectively) with little activity against other classes of proteases, including caspases, cathepsins, calpain, metalloproteases, and serine proteases (EC50s = > 100 μM).{24461,24462} 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.{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}  

 

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Description

A trisubstituted thiophene that selectively inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 μM, respectively); accelerates the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 =11 μM)

Formal name: 1-[5-[(2,3-dichlorophenyl)thio]-4-nitro-2-thienyl]-ethanone

Synonyms:  P5091

Molecular weight: 348.2

CAS: 882257-11-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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