GNE-6776

SKU: orb1302696

Description

GNE-6776 is a potent and selective small molecule inhibitor of the deubiquitinase USP7. It is a valuable research tool for probing USP7 biology in vitro and has been utilized in studies investigating oncology and neurodegenerative disease pathways.

Research Area

Cell Biology, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 2009273-71-4
• MW: 348.4
• Purity: 98.20% (May vary between batches)
• Formula: C₂₀H₂₀N₄O₂
• SMILES: CCc1c(cnc(N)c1-c1ccc(O)cc1)-c1ccc(nc1)C(=O)NC
• Target: DUB
• Solubility: DMSO:310 mg/mL (889.78 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (14.35 mM)

Bioactivity

• In Vivo:
  Although efficacious exposure is only transiently achieved, GNE-6776 causes modest, although significant, EOL-1 xenograft growth delay.
• In Vitro:
  GNE-6776 non-covalently targets USP7 12 distant from the catalytic cysteine. GNE-6776 attenuates ubiquitin binding and thus inhibits USP7 deubiquitinase activity. GNE-6776 interacts with acidic residues that mediate hydrogen-bond interactions with the ubiquitin Lys48 side chain. GNE-6776 targets cellular USP7, MDM2, and p53 signalling pathways.GNE-6776 selectively inhibits recombinant USP7 relative to 36 other deubiquitinases. GNE-6776 remains selective even at 100 μM, a more than sixfold higher concentration than used in cellular assays. GNE-6776 significantly inhibits USP7 while remaining selective against 44-47 other detected deubiquitinases.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, GEN-6776, GEN6776, GEN 6776, GNE6776, GNE 6776, GNE-6776, inhibit, Deubiquitinase, DUBs, USP7

Compound Identifiers

PubChem CID

122531750