HET0016

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^[1][2]. IC50 & Target:17.7 nM (CYP4A1), 12.1 nM (CYP4A2), 20.6 nM (CYP4A3)^[1], CYP450^[2] In Vitro:HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A ^[1].
HET0016 (100 μM; 24 hours, 48 hours) decreases migration and invasion of breast cancer metastatic cells ^[2].
In Vivo:HET0016 (10 mg/kg/day; i.v.; for 3 weeks) reduces tumor volume and lung metastasis in an immunocompetent breast cancer mouse model^[2].
HET0016 reduces the metalloproteinases’ levels in the lungs via PI3K/AKT pathway in mice^[2].
HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs population in lung microenvironment^[2].
HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junction proteins^[3].