Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : PFI-7
Catalog No.: PC-22417Not For Human Use, Lab Use Only.
PFI-7 is a potent, selective and cell-active chemical probe inhibitor for GID4, a substrate-binding receptor within the C-terminal to LisH (CTLH) E3 ligase complex.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
PFI-7 is a potent, selective and cell-active chemical probe inhibitor for Glucose-Induced Degradation 4 (GID4), the substrate receptor of the CTLH ubiquitin ligase complex, antagonizes Pro/N-degron binding to human GID4 with SPR Kd of 79 nM.
PFI-7 can directly displace the Pro/N-degron peptide PGLWKS from the GID4-binding pocket in a peptide displacement assay (Kdisp=4.1 uM).
PFI-7 binds within the β-barrel of GID4 substrate binding pocket, disrupting its interaction with the canonical Pro/N-degron peptide in cells.
PFI-7 decreases GID4-HaloTag binding to PGLKWS-NanoLuc on human embryonic kidney 293T (HEK293T) cells with IC50 of 0.54 uM.
PFI-7 is a suitable tool compound for use in cellular studies to interrogate GID4-mediated recruitment to the CTLH complex.
The Pro/N-degron pathway is a recently identified pathway that recognizes N-terminal degrons containing unmodified Proline residues (Pro/N-degrons).
| M.Wt | 401.51 | |
| Formula | C24H27N5O | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
1. Owens DDG, et al. Nat Chem Biol. 2024 May 21. doi: 10.1038/s41589-024-01618-0.
2. Yazdi AK, et al. RSC Med Chem. 2024 Mar 5;15(3):1066-1071.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
