inactivator

Piperonylic acid (2H-1,3-benzodioxole-5-carboxylic acid) is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic acid selectively inactivate the CYP73A P450 subpopulation.

Benzoylphenylalanine (LBPA) can be used as a photoaffinity peptide inactivator.

Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).

1. Linderane was characterized as a mechanism-based inactivator of CYP2C9.