PFI 7 is a selective GID4 antagonist (Kd = 80 nM by SPR assays and EC50 = 0.6 μM by cell-based NanoBRET). PFI 7 binds within the ?-barrel of GID4 substrate binding pocket, disrupting its interaction with the canonical Pro/N-degron peptide in live cells. It alters protein levels of several proteins including RNA helicases as measured by quantitative proteomics.
- Nom chimique ou matériau
- N-((1s,4s)-4-(1H-Benzo[d]imidazol-2-yl)cyclohexyl)-2-(((1H-indol-2-yl)methyl)amino)acetamide dihydrochloride
- Cible
- Ubiquitin Ligase (E3) Inhibitors
- Formule moléculaire
- C24H27N5O.2HCl
- Pureté
- 0.98
