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GNE-6640

Catalog No. T5461   CAS 2009273-67-8

GNE-6640 is a 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 USP43 and Ub-MDM2, respectively.

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GNE-6640 Chemical Structure
GNE-6640, CAS 2009273-67-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 64.00
2 mg In stock $ 93.00
5 mg In stock $ 155.00
10 mg In stock $ 263.00
25 mg In stock $ 563.00
50 mg In stock $ 812.00
100 mg In stock $ 1,130.00
1 mL * 10 mM (in DMSO) In stock $ 169.00
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Purity: 99.59%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GNE-6640 is a 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 USP43 and Ub-MDM2, respectively.
Targets&IC50 Ub-MDM2:0.23 μM, USP7 catalytic domain:0.43 μM , full length USP7:0.75 μM , full length USP43:20.3 μM
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.
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

Solubility Information

DMSO: 5 mg/mL (15.13 mM)

TargetMolReferences and Literature

1. Kategaya L, et al. USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. 2017 Oct 26;550(7677):534-538.

Related compound libraries

This product is contained In the following compound libraries:
Target-Focused Phenotypic Screening Library Anti-Aging Compound Library NO PAINS Compound Library Anti-Cancer Compound Library DNA Damage & Repair Compound Library Cell Cycle Compound Library Ubiquitination Compound Library Bioactive Compounds Library Max HIF-1 Signaling Pathway Compound Library Covalent Inhibitor Library

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GSK2643943A USP7-IN-1 EOAI3402143 SJB3-019A USP30 inhibitor 11 Spautin-1 DUB-IN-1 USP7-IN-8

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Keywords

GNE-6640 2009273-67-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Deubiquitinase DUBs inhibit Inhibitor GNE 6640 GNE6640 inhibitor

 

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