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GNE-6640
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.
Catalog No. T5461Cas No. 2009273-67-8
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Purity:98.64%
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GNE-6640
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $38 | In Stock | |
| 5 mg | $93 | In Stock | |
| 10 mg | $158 | In Stock | |
| 25 mg | $338 | In Stock | |
| 50 mg | $487 | In Stock | |
| 100 mg | $678 | In Stock | |
| 200 mg | $913 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $101 | In Stock |
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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 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (15.13 mM) | ||||||||||||||||||||
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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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