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LOXL2-IN-1 hydrochloride is a selective LOXL2 inhibitor with an IC50 of 126 nM.

LOXL2-IN-1 is shown to be selective for LOXL2 over LOX and three other amine oxidases (MAO-A, MAO-B and SSAO). In the human whole blood LOXL2 assay, LOXL2-IN-1 has an IC50 of 1.45 µM compared to 126 nM in the absence of blood proteins. LOXL2-IN-1 shows a 31-fold selectivity for LOXL2+BSA (IC50=190 nM) over LOX+BSA (IC50=5.91 µM). Against a panel of non-LTQ-containing AO enzymes (MAO-A, MAO-B and SSAO), LOXL2-IN-1 is found to be inactive at 30 µM. LOXL2-IN-1 is profiled for the inhibition of three different CYP enzymes (CYPs 3A4, 2C9 and 2D6) and in each case the IC50 is more than 30 µM[1].

[1]. Hutchinson JH, et al. Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX. ACS Med Chem Lett. 2017 Mar 1;8(4):423-427.

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