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GNE-6640
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Catalog No. T5461Cas No. 2009273-67-8
GNE-6640 is a non-covalent inhibitor targeting ubiquitin specific peptidase 7 (USP7), exhibiting IC50 values of 0.75 μM for full-length USP7, 0.43 μM for the USP7 catalytic domain, 20.3 μM for full-length USP43, and 0.23 μM for Ub-MDM2, respectively.
GNE-6640
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Purity: 98.64%
Catalog No. T5461Cas No. 2009273-67-8
GNE-6640 is a non-covalent inhibitor targeting ubiquitin specific peptidase 7 (USP7), exhibiting IC50 values of 0.75 μM for full-length USP7, 0.43 μM for the USP7 catalytic domain, 20.3 μM for full-length USP43, and 0.23 μM for Ub-MDM2, respectively.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $64 | In Stock | In Stock | |
| 2 mg | $93 | In Stock | In Stock | |
| 5 mg | $155 | In Stock | In Stock | |
| 10 mg | $263 | In Stock | In Stock | |
| 25 mg | $563 | In Stock | In Stock | |
| 50 mg | $812 | - | In Stock | |
| 100 mg | $1,130 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $169 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.64%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | GNE-6640 is a non-covalent inhibitor targeting ubiquitin specific peptidase 7 (USP7), exhibiting IC50 values of 0.75 μM for full-length USP7, 0.43 μM for the USP7 catalytic domain, 20.3 μM for full-length USP43, and 0.23 μM for Ub-MDM2, respectively. |
| Targets&IC50 | USP7 catalytic domain:0.43 μM , Ub-MDM2:0.23 μM, USP7 (full length):0.75 μM , USP43 (full length):20.3 μM |
| In vitro | GNE-6640 facilitates the promotion of endogenous MDM2 ubiquitination utilizing Lys48 (K48)-linked polyubiquitin chains leading to its proteasomal degradation. This compound specifically acts on cellular USP7, MDM2, and p53 signaling pathways, reducing the viability of 108 cell lines with IC50 values of ≤ 10 μM. When combined with DNA-damaging agents like doxorubicin or cisplatin, GNE-6640 activates the p53 response, thereby enhancing USP7 inhibitor efficacy and inducing tumor cell death. Furthermore, GNE-6640 augments cytotoxicity when used alongside various chemotherapeutic agents and targeted compounds, such as PIM kinase inhibitors, showcasing its potential as a versatile adjunct in cancer therapy. |
| Molecular Weight | 330.38 |
| Formula | C20H18N4O |
| Cas No. | 2009273-67-8 |
| Smiles | CCc1c(cnc(N)c1-c1ccc(O)cc1)-c1ccc2[nH]ncc2c1 |
| Relative Density. | 1.308 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (15.13 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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