Product Introduction
Bioactivity


英文名: GNE-6776

描述: GNE-6776 是一种具有口服活性的选择性USP7抑制剂。

体外活性: 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.

体内活性: 尽管有效曝露仅短暂实现，GNE-6776仍能引起适度但显著的EOL-1异种移植瘤生长延迟。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 310 mg/mL


关键字: GEN-6776 | Deubiquitinase | DUBs | GEN 6776 | Inhibitor | GNE-6776 | inhibit | GNE 6776 | GNE6776

相关产品: PR-619 | USP8-IN-3 | FT671 | HBX 19818 | RA-9 | USP5-IN-1 | MF-094 | DUB-IN-3 | USP22-IN-1 | B-AP15

相关库: Anti-Aging Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Cancer Compound Library | Ubiquitination Compound Library | Inhibitor Library | DNA Damage & Repair Compound Library | Orally Active Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library