Chemical Name |
HET0016 |
CAS Number |
339068-25-6 |
MDL Number |
MFCD00277704 |
Molecular Formula |
C12H18N2O |
Molecular Weight |
206.28 |
Introduction of 339068-25-6 :
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].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.