P22077

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WARNING: This product is for research use only, not for human or veterinary use.

Description:P22077 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor. P22077 potently induces apoptosis in 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 also significantly augmented the cytotoxic effects of doxorubicin (Dox) and etoposide (VP-16) in NB cells with an intact USP7-HDM2-p53 axis. Moreover, P22077 was found to be able to sensitize chemoresistant LA-N-6 NB cells to chemotherapy. In an in vivo orthotopic NB mouse model, P22077 significantly inhibited the xenograft growth of three NB cell lines. USP7-specific inhibitors like P22077 may serve not only as a stand-alone therapy but also as an effective adjunct to current chemotherapeutic regimens for treating NB with an intact USP7-HDM2-p53 axis.

Price and Availability

P22077, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406569Name: P22077CAS#: 1247819-59-5Chemical Formula: C12H7F2NO3S2Exact Mass: 314.98354Molecular Weight: 315.31Elemental Analysis: C, 45.71; H, 2.24; F, 12.05; N, 4.44; O, 15.22; S, 20.34

Synonym:P22077; P-22077; P 22077.

IUPAC/Chemical Name:1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone

InChi Key:RMAMGGNACJHXHO-UHFFFAOYSA-N

InChi Code:InChI=1S/C12H7F2NO3S2/c1-6(16)11-5-9(15(17)18)12(20-11)19-10-3-2-7(13)4-8(10)14/h2-5H,1H3

SMILES Code:CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O

Technical Data

Additional Information

References

1: Fan YH, Cheng J, Vasudevan SA, Dou J, Zhang H,Patel RH, Ma IT, Rojas Y, ZhaoY, Yu Y, Zhang H, Shohet JM, Nuchtern JG, Kim ES, Yang J. USP7 inhibitorP22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis. CellDeath Dis. 2013 Oct 17;4:e867. doi: 10.1038/cddis.2013.400. PubMed PMID:24136231; PubMed Central PMCID: PMC3920959.

2: Dar A, Shibata E, Dutta A. Deubiquitination of Tip60 by USP7determines the activity of the p53-dependent apoptotic pathway. Mol Cell Biol. 2013 Aug;33(16):3309-20. doi: 10.1128/MCB.00358-13. Epub 2013 Jun 17. PubMedPMID: 23775119; PubMed Central PMCID: PMC3753911.

3: Altun M, Kramer HB, Willems LI, McDermott JL, Leach CA, GoldenbergSJ, Kumar KG, Konietzny R, Fischer R, Kogan E, Mackeen MM, McGouran J,Khoronenkova SV, Parsons JL, Dianov GL, Nicholson B, Kessler BM. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylatingenzymes. Chem Biol. 2011 Nov 23;18(11):1401-12. doi: 10.1016/j.chembiol.2011.08.018.PubMed PMID: 22118674.