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GNE-6640

SKU: orb1301772

Description

GNE-6640 is a potent and selective non-covalent inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 0.75 µM for the full-length enzyme. This compound is a valuable chemical probe for studying USP7's role in oncology and p53 pathway regulation in both cellular and biochemical assays.

Research Area

Cell Biology, Molecular Biology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number2009273-67-8
MW330.38
Purity99.59%
FormulaC20H18N4O
SMILESCCc1c(cnc(N)c1-c1ccc(O)cc1)-c1ccc2[nH]ncc2c1
TargetDUB
SolubilityDMSO:5 mg/mL (15.13 mM)

Bioactivity

Target IC50
Ub-MDM2:0.23 μM|USP7 catalytic domain:0.43 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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

USP7, DUBs, Deubiquitinase, inhibit, Inhibitor, GNE6640, GNE-6640, GNE 6640

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    C20H18N4O

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Key Properties

No computed properties available.

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Protocol Information

GNE-6640 (orb1301772)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 110.00
2 mg
$ 140.00
5 mg
$ 200.00
1 ml x 10 mM (in DMSO)
$ 210.00
10 mg
$ 310.00
25 mg
$ 610.00
50 mg
$ 860.00
100 mg
$ 1,170.00
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