HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis). HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.

HET0016 (100 μM; 24 hours, 48 hours) decreases migration and invasion of breast cancer metastatic cells .HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A .

HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs population in lung microenvironment. HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junction proteins.HET0016 (10 mg/kg/day; i.v.; for 3 weeks) reduces tumor volume and lung metastasis in an immunocompetent breast cancer mouse model. HET0016 reduces the metalloproteinases' levels in the lungs via PI3K/AKT pathway in mice.

339068-25-6

C12H18N2O

206.28

DCM:12.5 mg/mL (60.60 mM),Need ultrasonic
DMSO:5 mg/mL (24.24 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years