P 22077 Chemical Properties

Melting point:

146 - 148°C

Boiling point:

395.4±42.0 °C(Predicted)

Density 

1.53±0.1 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO (up to 25 mg/ml)

form 

solid

color 

Off-white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

P 22077 Usage And Synthesis

Description

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

Uses

P22077 is an analog of the ubiquitin-specific protease (USP7) inhibitor P5091. It inhibits USP7, as well.

storage

Store at +4°C

References

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?17?823

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