P22077

SKU: orb1305502

Description

P 22077 is a small molecule inhibitor of the deubiquitinase USP7 (UniProt ID P22077) with an EC50 of 8.6 µM, and it also potently targets USP47. This compound is a valuable research tool for probing the roles of these enzymes in cellular processes such as the p53 pathway, DNA damage response, and Wnt signaling, both in vitro and in vivo.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 1247819-59-5
• MW: 315.32
• Purity: >98%
• Formula: C₁₂H₇F₂NO₃S₂
• SMILES: CC(=O)c1cc(c(Sc2ccc(F)cc2F)s1)[N+]([O-])=O
• Target: DUB (Deubiquitinating enzyme)
• Solubility: Soluble in DMSO (up to 25 mg/ml)

Bioactivity

• Target IC50:
  USP7:8.6 μM(EC50)
• In Vivo:
  P22077, administered at concentrations of 15-45 mM to cell lysates, inhibits a subset of DUBs (deubiquitinating enzymes) and prompts tumor cell death with an EC50 in the low micromolar range. Treatment with P22077 during the release from a G1/S arrest induced by hydroxyurea in U2OS cells results in a dose-dependent decrease in claspin protein levels, accompanied by reduced phosphorylation of serine 317 on Chk1. Furthermore, after P22077 exposure, quantitative mass spectrometry reveals diminished levels of E3 ubiquitin ligase components RBX1, DCAF7, DCAF11, and DNA damage-binding protein 1. While displaying negligible activity against DEN1 and SENP2 core, P22077 robustly inhibits USP7 with an IC50 of 8 μM, indicating selective inhibition towards USP7 and closely related DUB, USP47, over a range of DUBs, cysteine proteases, and other protease families in vitro.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Deubiquitinase, DUBs, Inhibitor, inhibit, USP2, USP7, USP4, USP47, USP5, P22077, P-22077, P 22077

Compound Identifiers

PubChem CID

46931953