lox-in-3

LOX-IN-3, an orally active inhibitor of lysyl oxidase (LOX), holds potential application in the fields of fibrosis, cancer, and angiogenesis research[1].

LOX-IN-3 dihydrochloride, an inhibitor of lysyl oxidase (LOX), inhibits bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM) activities.

COX-2 5-LOX-IN-3 (compound 5b) is a powerful dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively, showing promise for the investigation of inflammatory diseases [1].

LOX-IN-3 dihydrochloride monohydrate (Compound 33) is an orally active lysyl oxidase (LOX) inhibitor, intended for research in fibrosis, cancer, and angiogenesis [1].

COX-2 15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2 and 15-LOX with inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM, respectively. This compound effectively suppresses LPS-induced production of pro-inflammatory cytokines (IL-6, ROS, and NO), exhibiting targeted anti-inflammatory effects [1].

Compound 3, known as 5-LOX MAOs-IN-1, acts as an inhibitor of 5-LOX MAOs and is an effective free radical scavenger, displaying antioxidant characteristics. It has demonstrated neuroprotective effects in cell models damaged by oxidative stress and is capable of activating the neurogenesis microenvironment in adult mouse neural stem cells. This compound is utilized in research focused on neurodegenerative diseases.

BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 μM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 μM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 μM). BX-320 (200 mg/kg) inhibits the growth of lung tumors in a LOX melanoma mouse model of blood-borne metastasis. 1.Feldman, R.I., Wu, J.M., Polokoff, M.A., et al.Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1J. Biol. Chem.280(20)19867-19874(2005)

Masoprocol (meso-Nordihydroguaiaretic acid) is a potent, orally active lipoxygenase inhibitor that exhibits antihyperglycemic activity, making it potentially valuable for type II diabetes research. In vivo, Masoprocol reduces glucose and hepatic triglyceride concentrations [1] [2] [3].

Angiotensin II human TFA, a potent vasoconstrictor within the renin angiotensin system, plays a pivotal role in human blood pressure regulation primarily through interactions with the G-protein-coupled receptors Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). It not only prompts sympathetic nervous stimulation, aldosterone biosynthesis, and renal effects but also fosters growth in vascular smooth muscle cells and boosts collagen type I and III synthesis in fibroblasts. This action results in the thickening of the vascular wall and myocardium, alongside fibrosis. Additionally, Angiotensin II human TFA triggers apoptosis and encourages capillary formation from endothelial cells through the LOX-1 dependent redox-sensitive pathway [1] [2] [3] [4].

Phenethyl ferulate (Caffeic Acid 3-Methyl Phenethyl Ester) has chemopreventive properties against chemically induced colon carcinogenesis. It enhances apoptosis in azoxymethane induced colon tumors. It shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively.

Selaginellin has a neuroprotective effect against L-glutamate-induced neurotoxicity through mechanisms related to anti-oxidation and anti-apoptosis via scavenging reactive oxygen species and up-regulating the expression of klotho gene. Selaginellin shows