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

LOX:<1 μM(human), LOX:<10 μM(bovine)

LOX-IN-3 (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC 50 values of <10 μM and <1 μM, respectively. LOX-IN-3 is less active against SSAO/VAP-1 and MAO-B activities[1].

In young male Wistar rats, a single high (30 mg/kg) dose of LOX-IN-3 (Compound 33) completely abolishes lysyl oxidase activity. While plasma concentrations of LOX-IN-3 are far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta)[1]. In a 14-day unilateral ureteric obstruction (UUO) model, LOX-IN-3 (Compound 33, 10 mg/kg daily; orally) treatment increases kidney weight and thickness and reduces the area of fibrosis as measured by Picrosirius Red[1]. In BALB/c mice bearing hepatic fibrosis, LOX-IN-3 (Compound 33, 20 mg/kg daily, i.p.) treatment significantly reduces liver fibrosis. At the end of week 4 a mouse breast cancer cell line (4tl) is injected orthotopically. LOX-IN-3 (Compound 33) treatment significantly reduces liver fibrosis, collagen cross-links and the metastatic load in the liver[1].