A dual inhibitor of USP7 and USP47 (EC50s = 8.01 and 8.74 µM

P22077 – 5 mg

Brand:
Cayman
CAS:
1247819-59-5
Storage:
-20
UN-No:
Non-Hazardous - /

P22077 is a dual inhibitor of the deubiquitylating enzymes ubiquitin-specific protease 7 (USP7) and USP47 (EC50s = 8.01 and 8.74 µM, respectively, in a fluorescence-based enzyme assay).{27951} It is selective for USP7 and USP47 over other USPs and proteases with EC50 values greater than 50 µM. P22077 (25 µM) induces the accumulation of polyubiquitinated proteins in HEK293 cells. In neuroblastoma cells in vitro, P22077 blocks deubiquitylation of HDM2, a protein that normally deubiquitinates the tumor suppressor p53 leading to its degradation.{39388} When used at concentrations of 10 and 20 µM, it amplifies the cytotoxicity and p53-mediated apoptosis of doxorubicin (Item No. 15007) and etoposide (Item No. 12092) in neuroblastoma cells. P22077 inhibits tumor growth in neuroblastoma mouse xenograft models when administered at a dose of 20 mg/kg per day.  

 

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SKU: 23704 - 5 mg Category:

Description

A dual inhibitor of USP7 and USP47 (EC50s = 8.01 and 8.74 µM, respectively); selective for USP7 and USP47 over other USPs and proteases with EC50 values greater than 50 µM; induces the accumulation of polyubiquitinated proteins in HEK293 cells when used at a concentration of 25 µM; amplifies the cytotoxicity and p53-mediated apoptosis of doxorubicin of doxorubicin and etoposide in neuroblastoma cells when used at concentrations of 10 and 20 µM; inhibits tumor growth in neuroblastoma mouse xenograft models when administered at a dose of 20 mg/kg per day

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

Synonyms: 

Molecular weight: 315.3

CAS: 1247819-59-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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