产品说明

一般描述

A cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC₅₀ = 8.01 & 8.74 µM, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 (Cat. No. 662141) targets (IC₅₀ >50 µM). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 µM; 0.5 to 20 h), however PR619 treatment results in upregulation of both K⁴⁸- and K⁶³-linked, while P22077 exposure results in mainly enrichment of K⁴⁸-linked polyUb chains.
A cell-permeable thiophenylethanone compound that acts a direct, reversible, and selective inhibitor of deubiquitylating enzymes (DUBs) USP7 and USP47 (IC₅₀ = 8.01 & 8.74 µM, respectively). Exhibits only a minimal effect on other DUBs and proteases (>25 µM). Also shown to block UCH-L5 activity in HEK293T cell extracts, but not in intact cells. Stabilizes p53, HDM2, and p21 levels in HEK293T and HCT-116 cells and induces growth arrest (50% cytotoxicity concentration; CC₅₀ = 16.6 and 7.83 µM).

Note: A pan-DUB selective inhibitor PR-619 (Cat. No. 662141) is also available.

包装

25 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Altun, M., et al. 2011. Chem. Biol.18, 1401.
Tian, X., et al. 2011. Assay Drug Dev. Technol.9, 165.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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