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GNE-6776 is a selective USP7 inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $74 | In Stock | |
5 mg | $178 | In Stock | |
10 mg | $287 | In Stock | |
25 mg | $552 | In Stock | |
50 mg | $793 | In Stock | |
100 mg | $1,080 | In Stock | |
1 mL x 10 mM (in DMSO) | $197 | In Stock |
Description | GNE-6776 is a selective USP7 inhibitor. |
In vitro | GNE-6776 non-covalently targets USP7 12?? distant from the catalytic cysteine. GNE-6776 attenuates ubiquitin binding and thus inhibits USP7 deubiquitinase activity. GNE-6776 interacts with acidic residues that mediate hydrogen-bond interactions with the ubiquitin Lys48 side chain. GNE-6776 targets cellular USP7, MDM2, and p53 signalling pathways.GNE-6776 selectively inhibits recombinant USP7 relative to 36 other deubiquitinases. GNE-6776 remains selective even at 100?μM, a more than sixfold higher concentration than used in cellular assays. GNE-6776 significantly inhibits USP7 while remaining selective against 44-47 other detected deubiquitinases. |
In vivo | Although efficacious exposure is only transiently achieved, GNE-6776 causes modest, although significant, EOL-1 xenograft growth delay. |
Alias | GEN6776 |
Molecular Weight | 348.4 |
Formula | C20H20N4O2 |
Cas No. | 2009273-71-4 |
Smiles | CCc1c(cnc(N)c1-c1ccc(O)cc1)-c1ccc(nc1)C(=O)NC |
Relative Density. | 1.242 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO: 310 mg/mL |
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