Biological Activity
Sulfopin is a covalent PIN1 inhibitor used to study prolyl-isomerase signaling and MYC-driven cancer biology. Sulfopin covalently targeted PIN1 Cys113 and showed selective cellular engagement.
In Vitro
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| PIN1 engagement | Biochemical and two independent chemoproteomic approaches. [1] | Sulfopin covalently targeted PIN1 Cys113 and showed selective cellular engagement. |
| Proliferation boundary | Cancer-cell panel and MYC transcriptional analyses. [1] | PIN1 inhibition produced modest viability effects in many lines despite lower MYC-associated transcription. |
| Apoptosis assessment | PATU-8988T cells; 1 or 2.5 µM for 5–6 days. [1], Extended Data apoptosis experiments | The reported assays did not show caspase-3 activation; PIN1 protein abundance was unchanged. Target engagement did not guarantee acute apoptosis. |
In Vivo
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Tumor-model response | MYCN-driven neuroblastoma mouse/zebrafish and murine pancreatic-cancer models. [1] | Reduced tumor progression and survival benefits were reported in these settings. |
Interpretation
PIN1 engagement does not guarantee rapid cytotoxicity in every cell line.
