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P5091
Cat. No. PI-100
Structure:
1-[5-[(2,3-Dichlorophenyl)thio]-4-nitro-2-thienyl]ethanone
Activity:
Ubiquitin specific protease 7 (USP7) inhibitor
P5091 is a selective and inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 4.2 μM. P5091 displays little or no inhibition of other USP variants or proteases such as caspase, cathepsins and serine proteases but does have some activity at USP47. P5091 induces elevated p53 and apoptosis in cancer cell lines and possesses antiangiogenic activity in vivo.
Weinstock et al (2012) Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47. J.Med.Chem. 3 789 PMID: 24900381
Chauhan et al (2012) A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell 22 345 PMID: 22975377
Related areas
All small molecules >
All deubiquitinating enzyme modulators >
All cancer research categories >
Technical Data
| Structure | 1-[5-[(2,3-Dichlorophenyl)thio]-4-nitro-2-thienyl]ethanone |
| CAS Number | 882257-11-6 |
| Molecular Weight | 348.22 |
| Formula | C12H7Cl2NO3S2 |
| Sequence | 1-[5-[(2,3-Dichlorophenyl)thio]-4-nitro-2-thienyl]ethanone |
Solubility and Storage
| Solubility | Soluble to 10 mM in DMSO |
| Appearance | Off-white solid |
| Storage | Store desiccated, frozen and in the dark |
Batch Specific Data
| Purity | ≥98% (HPLC) |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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