Drug intelligence / Profile preview

HET0016

Development stage
Preclinical
Lead developer
Augusta University
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
01

Overview

HET0016 (N-hydroxy-N'-(4-butyl-2-methylphenyl)formamidine) is a potent and selective small molecule inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis. It primarily acts by inhibiting enzymes in the cytochrome P450 4A (CYP4A) and 4F (CYP4F) families, which are responsible for the omega-oxidation of arachidonic acid to 20-HETE. 20-HETE is a bioactive lipid that plays a significant role in promoting tumor cell proliferation, migration, and neovascularization. In preclinical studies, HET0016 has been shown to reduce tumor aggressiveness, inhibit angiogenesis, and disrupt vascular mimicry in models of glioblastoma and triple-negative breast cancer. It also appears to modulate the IL-8/CXCR2 signaling pathway, further contributing to its anti-tumor effects.

Other names
N-hydroxy-N'-(4-butyl-2-methylphenyl)formamidineN-hydroxy-N'-(4-butyl-2-methylphenyl)methanimidamide
02

Targets

COXCYP2C/CYP2J (Cytochrome P450 2C and 2J epoxygenase)CYP4F2 (Cytochrome P450 family 4 subfamily F member 2)CYP4A (Cytochrome P450 4A family)CYP4A11 (Cytochrome P450 family 4 subfamily A member 11)CYP3A4 (Cytochrome P450 3A4)CYP4F3CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)

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