LOX-IN-3 dihydrochloride

SKU: orb1303455

Description

LOX-IN-3 dihydrochloride is a small molecule inhibitor of lysyl oxidase (LOX) and LOXL2, demonstrating potent activity with IC50 values below 10 μM and 1 μM for the bovine and human enzymes, respectively. This compound is a valuable research tool for studying extracellular matrix remodeling, fibrosis, and cancer metastasis in both cellular and animal models.

Research Area

Metabolism Research, Neuroscience

Key Properties

• CAS Number: 2409964-23-2
• MW: 353.24
• Purity: 99.86% (May vary between batches)
• Formula: C₁₃H₁₅Cl₂FN₂O₂S
• SMILES: Cl.Cl.NC\C=C(/F)CS(=O)(=O)c1cccc2cccnc12
• Target: Lipoxygenase,Monoamine Oxidase
• Solubility: DMSO:55 mg/mL (155.7 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.66 mM)

Bioactivity

• Target IC50:
  LOX:<1 μM(human)|LOX:<10 μM(bovine)
• In Vivo:
  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). 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. 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.
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• In Vitro:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LOX, LOX IN 3 dihydrochloride, LOX-IN-3, LOXIN3 dihydrochloride, LOX-IN-3 Dihydrochloride, LOXL2, inhibit, PXS-5505 (hydrochloride), oxidase, lysyl, Inhibitor, Monoamine Oxidase, MAO, fibrosis

Compound Identifiers

PubChem CID

146317832