Cat. No. Name Size Price Add Cart
KI2401P2207710 mg$236
P2207750 mg$592

Chemical Characteristic

Product NameP22077
SynonymsN/A
CAS No.1247819-59-5
Molecular Weight 315.32
FormulaC12H7F2NO3S2
Chemical Name1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]ethanone
SmilesC(=O)(C)c1cc(c(s1)Sc1c(cc(cc1)F)F)[N](=O)O
Chemical Structure

Biological activities

P22077 is an ubiquitin-specific protease 7 (USP7) inhibitor. P22077 inhibits USP7 with an IC50 of 8 μM.[1] P22077 induces apoptosis in neuroblastoma (NB) cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. P22077 stabilizes p53 by inducing HDM2 protein degradation in NB cells. In an in vivo orthotopic NB mouse model, P22077 significantly inhibits the xenograft growth of three NB cell lines.[2]

References

[1] Tian X, et al. Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format. Assay Drug Dev Technol. 2011, 9(2): 165-173.
[2] Fan YH, et al. USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis. Cell Death Dis. 2013, 4: e867.

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