GNE-6640
CAS No. : 2009273-67-8
| Size | Price | Stock |
|---|---|---|
| 5mg | $190 | In-stock |
| 10mg | $320 | In-stock |
| 25mg | $680 | In-stock |
| 50mg | $1090 | In-stock |
| 100mg | $1750 | In-stock |
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| Cat. No. : | HY-112937 |
| M.Wt: | 330.38 |
| Formula: | C20H18N4O |
| Purity: | >98 % |
| Solubility: | DMSO : 5 mg/mL (ultrasonic) |
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].
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