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P22077 | Selective USP7 inhibitor

P22077 (1247819-59-5) is a selective (tested against 23 other DUBs) inhibitor of USP7 (IC50 = 8 µM) and the closely related USP47.1,2 It destabilizes claspin, a scaffolding protein involved in regulating Chk1 kinase, a DNA damage response enzyme.2 P22077 inhibits neuroblastoma growth via induction of p53-mediated apoptosis.3 N-Myc was destabilized by P22077 inhibition of USP7 in human neuroblastoma cells.4 It was able to stabilize p53 levels in conjunction with an Mdm2 inhibitor (Nutlin-3, Cat# 10-1350) in HCT116 colorectal carcinoma cells.5

References/Citations

1) Tian et al. (2011), Characterization of Selective Ubiquitin and Ubiquitin-like Protease Inhibitors Using a Fluorescence-Based Multiplex Assay Format; Assay Drug Dev. Technol. 9 165
2) Altun et al. (2011), Activity-based chemical proteomics accelerates inhibitor development for deubiquitinylating enzymes; Chem. Biol. 18 1401
3) Fan et al. (2013), USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis; Cell Death Dis. 4 e867
4) Tavana et al. (2016), HAUSP deubiquitinates and stabilizes M-Myc in neuroblastoma; Nat. Med. 22 1180
5) Tavana et al. (2018), Targeting HAUSP in both p53 wildtype and p53-mutant tumors; Cell Cycle May 15 epub 1

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Focus Biomolecules cell signaling reagent supplier, chemical structure P22077 | Selective USP7 inhibitor | CAS 1247819-59-5

Catalog#  10-4125-0010

$65.00
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CAS:
1247819-59-5
Catalog Number:
10-4125
Activity:
Selective USP7 inhibitor
Chemical Name:
1-(5-((2,4-Difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
Molecular Weight:
315.32
Molecular Formula:
C12H7F2NO3S2
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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