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GNE-6776

Catalog No. T4634   CAS 2009273-71-4
Synonyms: GEN6776

GNE-6776 is a selective USP7 inhibitor.

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GNE-6776, CAS 2009273-71-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 79.00
5 mg In stock $ 197.00
10 mg In stock $ 310.00
25 mg In stock $ 630.00
1 mL * 10 mM (in DMSO) In stock $ 197.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Synonyms GEN6776
Molecular Weight 348.406
Formula C20H20N4O2
CAS No. 2009273-71-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 310 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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:
NO PAINS Compound Library Orally Active Compound Library HIF-1 Signaling Pathway Compound Library Ubiquitination Compound Library DNA Damage & Repair Compound Library Anti-Cancer Compound Library Anti-Aging Compound Library Cell Cycle Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

Related Products

Related compounds with same targets
USP8-IN-2 USP8-IN-3 USP15-IN-1 IMP-1710 HBX 41108 LDN-91946 FT827 USP7-IN-6

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GNE-6776 2009273-71-4 Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB GNE6776 Deubiquitinase DUBs GEN6776 Inhibitor inhibit GNE 6776 inhibitor