1. Cell Cycle/DNA Damage
  2. Deubiquitinase

GNE-6640 

Cat. No.: HY-112937
Handling Instructions

GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.

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

GNE-6640 Chemical Structure

GNE-6640 Chemical Structure

CAS No. : 2009273-67-8

Size Price Stock
5 mg USD 210 Get quote
10 mg USD 350 Get quote
25 mg USD 740 Get quote
50 mg USD 1200 Get quote
100 mg USD 1950 Get quote

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.

IC50 & Target

IC50: 0.75 μM(full length USP7), 0.43 μM(USP7 catalytic domain), 20.3 μM(full length USP43), 0.23 μM(Ub-MDM2)[1].

In Vitro

GNE-6640 promotes endogenous MDM2 ubiquitination with Lys48 (K48)-linked polyubiquitin chains, which directs proteasomal degradation13. GNE-6640 targets cellular USP7, MDM2, and p53 signalling pathways. GNE-6640 decreases viability of 108 cell lines with IC50 ≤ 10 μM. Combining GNE-6640 with doxorubicin or cisplatin (DNA-damaging agents), which could activate the p53 response and enhance USP7 inhibitor efficacy. GNE-6640 could induce tumor cell death. GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 160 mg/mL (484.29 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0268 mL 15.1341 mL 30.2682 mL
5 mM 0.6054 mL 3.0268 mL 6.0536 mL
10 mM 0.3027 mL 1.5134 mL 3.0268 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.67 mg/mL (8.08 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.67 mg/mL (8.08 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.67 mg/mL (8.08 mM); Clear solution

References
Molecular Weight

330.38

Formula

C₂₀H₁₈N₄O

CAS No.

2009273-67-8

SMILES

OC1=CC=C(C2=C(CC)C(C3=CC4=C(NN=C4)C=C3)=CN=C2N)C=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GNE-6640
Cat. No.:
HY-112937
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GNE-6640

Cat. No.: HY-112937