Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors.In Vitro: MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days).
Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription.
Sulfopin (1, 2.5 μM; PATU-8988T cells; 4 days) shows a small but significant reduction in the number of synthesis (S)-phase cells and a corresponding increase of growth 1 (G1)-phase cells.In Vivo: Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice.
Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice.
Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish.