P22077

Catalog No.S7133

P22077 Chemical Structure

Molecular Weight(MW): 315.32

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

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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] USP47 [2] USP2 core [2] USP4 [2] USP5 [2]
8.6 μM(EC50) 8.74 μM(EC50) >50 μM(EC50) >50 μM(EC50) >50 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

Solubility (25°C)

In vitro DMSO 63 mg/mL (199.79 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 315.32
Formula

C12H7F2NO3S2

CAS No. 1247819-59-5
Storage powder
in solvent
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID