20 hete

20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway to increase FBXO10 expression.20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway.

20-HETE Inhibitor-1 (Comp 83) serves as an inhibitor of 20-HETE formation [1].

CAY10462 (CTK8E8405) is an effective and selective inhibitor of the 20-HETE synthase CYP4A11 with an IC50 of 8.8 nM. CAY10462 exhibits nearly 200 times less potent for 1A, 1C, and 3A CYP450 enzymes.

(±)18-HETE is the racemic version of a cytochrome P450 (CYP450) metabolite of arachidonic acid. When formed by the CYP2E1 isoform, 18-HETE is comprised 100% of the (R) isomer. 18(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, whereas 18(S)-HETE does not affect perfusion pressure. 18-HETE has negligible effects on ATPase activity. 18(R)-HETE at 1 μM completely blocks 20-HETE-induced vasoconstriction of renal arterioles.

20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-AA binds to isolated ligand binding domains of peroxisome proliferator-activated receptor α (PPARα) (Kd = 0.87 ± 0.12 μM) and PPARγ (Kd = 1.7 ± 0.5 μM), and is a dual activator of PPARα and PPARγ in a transiently transfected COS-7 cell reporter system.

CYP4A11 CYP4F2-IN-1 is a cytochrome P450 (CYP) 4A11 and CYP4F2 inhibitor, applicable for research on kidney, cardiovascular, and cerebrovascular diseases.

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) and a selective CYP450 inhibitor, shown to inhibit angiogenesis and tumor growth.

20-5,14-HEDGE, a 20-HETE analog, protects against lung ischemic reperfusion injury in rats [1].

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)

CYP4A11 CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50 values of 140 nM and 40 nM, respectively. Extractable from liver and kidney, CYP4A11 CYP4F2-IN-2 has the potential to treat kidney diseases.

CYP4A11 CYP4F2-IN-2 (compound 15) serves as an orally administered inhibitor targeting CYP4A11 4F2, exhibiting IC50 values of 120 nM and 220 nM, respectively. This compound effectively suppresses 20-HETE production within the rat kidney and shows promise in mitigating the progression of diabetic nephropathy and autosomal dominant polycystic kidney disease [1].

Squalane is a lipid found in some fish oils (especially shark liver oil) and some vegetable oils. It has anticancer and antioxidant properties and is used as a skin moisturizer and emollient.

20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).