GNE-6776

SKU: orb1225753

Description

GNE-6776 is a novel potent, specific, non-covalent, orally bioavailable USP7 inhibitor with IC50 of 1.34 uM ; dislpalys selectivity over USP47 and USP5 (>200 uM); promotes endogenous MDM2 ubiquitination, stabilized p53 and upregulated p21, induces tumour cell death and enhances cytotoxicity with chemotherapeutic agents; promotes on-target pathway modulation in human xenografts.

Key Properties

• CAS Number: 2009273-71-4
• MW: 348.406
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₀N₄O₂
• SMILES: CCC1=C(C(=NC=C1C2=CN=C(C=C2)C(=O)NC)N)C3=CC=C(C=C3)O
• Target: DUB
• Solubility: DMSO: ≥310 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Animal model: Immunodeficient C. B-17 SCID mice (aged 12-16 weeks) withEOL1 AML xenograft. Dosage: 100 or 200 mg/kg. Administration: Oral gavage on a once or twice daily schedule; for 10 days. Result: Significant EOL-1 xenograft growth inhibition.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GNE6776 | GNE 6776

Quick Database Links

Gene Symbol

DUB