[CAS NO. 2009273-67-8] GNE-6640
PRODUCTS SPECIFICATIONS [2009273-67-8]
DESCRIPTION [2009273-67-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 330.38 |
| Molecular Formula | C20H18N4O |
| SMILES | OC1=CC=C(C2=C(CC)C(C3=CC4=C(NN=C4)C=C3)=CN=C2N)C=C1 |
1 Publications Citing Use of MCE
Summary
GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7) , with IC 50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.
IC50 & Target
IC50: 0.75 μM(full length USP7), 0.43 μM(USP7 catalytic domain), 20.3 μM(full length USP43), 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 IC 50 ≤ 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 5 mg/mL ( 15.13 mM ; Need ultrasonic)
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 |
| 10 mM | 0.3027 mL | 1.5134 mL | 3.0268 mL |