The probe PFI-7 (hydrochloride) is available at Sigma and Tocris.
The inactive control PFI-7N (hydrochloride) is available at Sigma.
Probe | Negative control | |
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PFI-7 |
| PFI-7N |
Pfizer in collaboration with the SGC have developed PFI-7, a potent, cell active chemical probe for the E3 ligase GID4. PFI-7 binds potently to GID4 with KD = 0.08 μM (SPR) and displaces the known degron1 peptide in a NanoBRETTM assay with EC50 = 0.6 μM. PFI-7N is a closely related negative control with KD = 5 μM (SPR). A co-crystal structure has been deposited.
We have further developed a handle PFI-E3H1 and a PEGylated analogue to show that the handle tolerates a substitution. These findings offers opportunities to synthesize proximity-inducing or degrader modalities2.
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[PFI-7] (μM) | [PFI-7] (μM) |
A NanoBRET assay was used to show target engagement in cells.
The interaction was between NanoLuc® tagged degrons and full-length GID4.
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Main features