Sulfopin is a potent, selective and covalent inhibitor of Pin1 with Ki of 17 nM in FP assay, targets Pin1's active site Cys113, blocks Myc-driven tumors.
Sulfopin inhibits the catalytic activity of Pin1 with an apparent Ki of 211 nM in chymotrypsin-coupled peptidyl-prolyl isomerization assay.
Sulfopin is highly selective for Pin1 Cys113 over other 161 cysteine residues.
Sulfopin could phenocopy Pin1 knockout.
Sulfopin significantly resensitized HeLa cells to irradiation in a dose-dependent manner, and decreases IRAK1 Thr209 phosphorylation at concentrations as low as 100 nM.
Sulfopin (1 μM) shows a Pin1-dependent viability effect following long-term exposure.
Sulfopin downregulates Myc transcriptional activity and increases c-Myc protein levels in Mino B cells, blocks neuroblastoma in zebrafish.
Sulfopin (20 or 40 mg/kg) inhibits pancreatic cancer progression in mice, significantly extends survival.