2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. GNE-6640

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 USP47 and Ub-MDM2, respectively.

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GNE-6640 Chemical Structure

GNE-6640 Chemical Structure

CAS No. : 2009273-67-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 209 In-stock
Solution
10 mM * 1 mL in DMSO USD 209 In-stock
Solid
5 mg USD 190 In-stock
10 mg USD 320 In-stock
25 mg USD 680 In-stock
50 mg USD 1090 In-stock
100 mg USD 1750 In-stock
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Based on 3 publication(s) in Google Scholar

GNE-6640 Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

View All Isoforms
USP1 USP2 USP7 USP8 USP30 UCHL1

  • Biological Activity

  • Purity & Documentation

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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 USP47 and Ub-MDM2, respectively[1][2].

IC50 & Target

IC50: 0.75 μM (full length USP7), 0.43 μM (USP7 catalytic domain), 20.3 μM (full length USP47), 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].

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

GNE-6640 Related Antibodies
Molecular Weight

330.38

Formula

C20H18N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (15.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.93%

COA (247 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0268 mL 15.1341 mL 30.2682 mL 75.6704 mL
5 mM 0.6054 mL 3.0268 mL 6.0536 mL 15.1341 mL
10 mM 0.3027 mL 1.5134 mL 3.0268 mL 7.5670 mL
15 mM 0.2018 mL 1.0089 mL 2.0179 mL 5.0447 mL
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GNE-6640 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-66402009273-67-8GNE6640GNE 6640DeubiquitinaseDUBsInhibitorinhibitorinhibit

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