1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. GNE-6776

GNE-6776 

Cat. No.: HY-107986 Purity: 98.03%
Handling Instructions

GNE-6776 is a selective USP7 inhibitor.

For research use only. We do not sell to patients.

GNE-6776 Chemical Structure

GNE-6776 Chemical Structure

CAS No. : 2009273-71-4

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10 mM * 1 mL in DMSO USD 242 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

GNE-6776 is a selective USP7 inhibitor.

IC50 & Target

USP7[1]

In Vitro

GNE-6776 non-covalently targets USP7 12 Å 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[1].

In Vivo

Although efficacious exposure is only transiently achieved, GNE-6776 causes modest, although significant, EOL-1 xenograft growth delay[1].

Molecular Weight

348.40

Formula

C₂₀H₂₀N₄O₂

CAS No.

2009273-71-4

SMILES

CCC(C(C1=CC=C(O)C=C1)=C(N)N=C2)=C2C3=CC=C(C(NC)=O)N=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (287.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8703 mL 14.3513 mL 28.7026 mL
5 mM 0.5741 mL 2.8703 mL 5.7405 mL
10 mM 0.2870 mL 1.4351 mL 2.8703 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

EOL-1 cells are seeded into 384-well plates 24 h before compound addition. Cells are then incubated with compound (e.g., GNE-6776; 0.003, 0.009, 0.027, 0.082, 0.25, 0.74, 2.22, 6.67, and 20 μM) for 72 h or 120 h before assaying viability. Assays are performed in biological triplicate. Cells are incubated (37°C, 5% CO2) in RPMI-1640, 2.5% FBS (72 h assay) or 5% FBS (120 h assay), and 2 mM glutamine throughout the assay. The reported IC50 and mean viability metrics are as follows: IC50 is the dose at which the estimated inhibition is 50% relative to untreated wells (that is, absolute IC50). The mean viability is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
GNE-6776 is administered at 200 mg/kg (body weight) by oral gavage to female C.B-17 SCID mice, aged 12-16 weeks (n=3 per time point). No randomization is used for DMPK studies. At 0.5, 1, 2, 4, 8 and 24 h post-dose, blood samples are collected by terminal cardiac puncture into anticoagulant tubes (EDTA). Clarified plasma is then transferred to a fresh tube and snap frozen. GNE-6776 plasma concentrations are determined by LC-MS/MS[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

GNE-6776GNE6776GNE 6776DeubiquitinaseDUBsInhibitorinhibitorinhibit

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