CYP4 Inhibitor

Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC₅₀ values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.

20-HETE inhibitor-2 is an orally active 20-HETE inhibitor. 20-HETE inhibitor-2 can inhibit the activities of CYP4F2 and CYP4A11, thereby suppressing the production of 20-HETE. 20-HETE inhibitor-2 has the effect of improving blood glucose and can be used for the research of various diseases related to 20-HETE such as obesity.

ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with K_i values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity.

BM-51 is a selective inhibitor of CYP4Z1, with a human IC₅₀ value of 91.7 nM. BM-51 binds to amino acid residues of CYP4Z1, thereby inhibiting its enzymatic activity. BM-51 downregulates the protein expression of stem cell markers (ALDH1A1, SOX2, OCT3/4 and KLF4) in cancer cells, inhibits cancer cell migration and invasion, and exhibits low toxicity to normal cells/tissues. BM-51 suppresses tumor initiation capacity and enhances the chemotherapeutic efficacy of Doxorubicin (HY-15142A). BM-51 can be used in breast cancer-related research.

CYP4Z1-IN-3 is a selective CYP4Z1 inhibitor with a human IC₅₀ of 55.3 nM. CYP4Z1-IN-3 inhibits breast cancer cell migration and induces apoptosis. CYP4Z1-IN-3 can be used for the research of breast cancer.

CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC₅₀s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases.

CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC₅₀s of 19 nM and 17 nM, respectively. CYP4A11/CYP4F2-IN-1 has potential for the research of renal diseases.

CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC₅₀ of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo.

CYP4Z1-IN-2 (compound 7) is a reversible inhibitor of CYP4Z1 (K_i=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.