Biological Activity & Performance
| Endpoint | Model / source | Reported finding |
|---|---|---|
| Enzyme inhibition | Recombinant human PIN1 PPIase assay; Fig. 1 / Supplementary Table 2 [1] | IC50 640 nM; a biochemical endpoint. |
| Mechanism | PIN1-dependent responses [1] | Covalent inhibition accompanied PIN1 degradation, ROS generation and DNA damage. |
| Cellular activity | Cancer-cell models; Figs. 3–7 [1] | Reduced proliferation, invasion and cancer stem-cell phenotypes; cell-death markers increased. |
| Animal efficacy | MDA-MB-231 lung colonization; Fig. 7c [1] | Daily 5 mg/kg intraperitoneal treatment reduced metastatic growth compared with vehicle. |
| Tolerability | Mouse studies [1] | No gross organ toxicity was reported at the efficacy regimen; higher-dose studies showed injection-site toxicity. |
How to interpret the evidence
This experimental lung-colonization model is not spontaneous metastasis. Cellular effects combine PIN1 inhibition and oxidative/DNA-damage responses; they should not be attributed solely to PIN1 protein loss.