Home Ubiquitin DUB inhibitor P22077

P22077

Catalog No.S7133

For research use only.

P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.

P22077 Chemical Structure

CAS No. 1247819-59-5

Selleck's P22077 has been cited by 17 publications

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Biological Activity

Description P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.
Targets
USP7 [1]
(Cell-free assay)		 USP47 [2]
8.6 μM 8.74 μM(EC50)
In vitro

P22077 is an analog of the recently discovered USP7 inhibitor P5091. P22077 has negligible activity versus DEN1 and SENP2core over the concentration range tested, but inhibits USP7 with an IC50 of 8 μM. [1] The inhibitory activities of P22077 in vitro against a panel of DUBs, cysteine proteases, and other families of proteolytic enzymes demonstrate that P22077 inhibits USP7 and the closely related DUB USP47. P22077 inhibits a smaller subset of DUBs at a concentration of 15–45 mM in cell lysates. P22077 induces (tumor) cell death with EC50 values in the low micromolar range. P22077 inhibition exhibited changes in ubiquitylated protein levels that are distinct from the broad specificity inhibitor. P22077 treatment of U2OS cells during release from G1/S arrest induces with hydroxyurea resulted in a dose-dependent loss of claspin protein and a concomitant decrease in phospho Serine 317 Chk1. Furthermore, quantitative MS suggestes the E3 ubiquitin ligase components RBX1, DCAF7, DCAF11, and the DNA damage binding protein 1 (DDB1) to be reduced upon cellular treatment with P22077. [2]

Protocol (from reference)

Solubility (25°C)

In vitro

 DMSO 63 mg/mL
(199.79 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

 3mg/mL

Chemical Information

Molecular Weight 315.32
Formula

C12H7F2NO3S2
CAS No. 1247819-59-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)C1=CC(=C(S1)SC2=C(C=C(C=C2)F)F)[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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