DUB INHIBITOR VI P22077 1PC X 25MG (C005B-231741)

General description

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.

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 315.32. Empirical Formula: C₁₂H₇F₂NO₃S₂. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 50 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: CC(C1: CC([N+]([O-]): O): C(SC2: CC: C(F)C: C2F)S1): O. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.