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

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

LOX-IN-3 dihydrochloride monohydrate (Compound 33) is a lysyl oxidase (LOX) inhibitor with oral activity. It is specifically designed for research purposes in the areas of fibrosis, cancer, and angiogenesis [1].

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

COX-2/5-LOX-IN-3 (compound 5b) is a powerful and 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. This compound, COX-2/5-LOX-IN-3, shows promise for the investigation of inflammatory diseases [1].

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

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.

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)