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[1].
MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days)[1].Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription[1].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[1].
Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice[1].Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice[1].Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish[1].
[1]. Dubiella C, et al. Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 2021;17(9):954-963.