| Description | 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. |
| In vitro | 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 . |
| In vivo | 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. |
| Target activity | CYP4A1:17.7 nM , CYP4A2: 12.1 nM , CYP4A3: 20.6 nM |
| molecular weight | 206.28 |
| Molecular formula | C12H18N2O |
| CAS | 339068-25-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DCM: 12.5 mg/mL (60.60 mM), Sonication is recommended. DMSO: 5 mg/mL (24.24 mM), Sonication is recommended. |
| References | 1. Seki T, et al. Cytochrome P450 4A isoform inhibitory profile of N-hydroxy-N'-(4-butyl-2-methylphenyl)-formamidine (HET0016), a selective inhibitor of 20-HETE synthesis. Biol Pharm Bull. 2005 Sep;28(9):1651-4. 2. Borin TF, et al. HET0016 decreases lung metastasis from breast cancer in immune-competent mouse model. PLoS One. 2017 Jun 13;12(6):e0178830. 3. Liu Y, et al. The protective effect of HET0016 on brain edema and blood-brain barrier dysfunction after cerebral ischemia/reperfusion. Brain Res. 2014 Jan 28;1544:45-53. |