| Name | GNE-6640 |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 5 mg/mL (15.13 mM), Sonication is recommended.
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| Keywords | USP7 | Inhibitor | inhibit | GNE-6640 | GNE6640 | GNE 6640 | DUBs | Deubiquitinase |
| Inhibitors Related | P22074 | USP7-IN-4 | P 22077 | N-Ethylmaleimide | DUB-IN-1 | SJB3-019A | USP30 inhibitor 11 | Vialinin A | GRL0617 | Spautin-1 | USP8-IN-3 | 6-Thioguanine |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Ubiquitination Compound Library | HIF-1 Signaling Pathway Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Cell Cycle Compound Library | Anti-Cancer Compound Library |