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CYP4Z1-IN-2 (compound 7) is a reversible inhibitor of CYP4Z1 (Ki=2.2 μM), which inhibits the production of 14,15-EET in breast cancer cells. CYP4Z1-IN-2 inhibits the CYP4Z1-mediated Luc-BE O-debenzylation reaction with an IC50 of 5.9 μM[1].

CAY10770 is an inhibitor of the cytochrome P450 (CYP) isoform CYP4Z1 (IC50 = 5.9 μM).1 It is selective for CYP4Z1 over CYP4A11, CYP4F2, CYP4F3a, CYP4F3b (IC50s = 187-282 μM) but does inhibit CYP4F8 and CYP4F12 (IC50s = 167 and 91 μM, respectively). CAY10770 (3 μM) inhibits the production of 14(15)-EET, 19-HETE, and 14(15)-DiHET by 83, 86, and 80%, respectively, in T47D breast cancer cells expressing CYP4Z1.

CYP4Z1: 2.2 μM (Ki)

1.Kowalski, J.P., McDonald, M.G., Pelletier, R.D., et al.Design and characterization of the first selective and potent mechanism-based inhibitor of cytochrome P450 4Z1J. Med. Chem.63(9)4824-4836(2020)