Bioactivity | (2-Chloropyridin-4-yl)methanamine hydrochloride is a selective LOXL2 inhibitor with an IC50 of 126 nM. |
Target | IC50: 126 nM (LOXL2) |
Invitro | (2-Chloropyridin-4-yl)methanamine hydrochloride 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, (2-Chloropyridin-4-yl)methanamine hydrochloride has an IC50 of 1.45 µM compared to 126 nM in the absence of blood proteins. (2-Chloropyridin-4-yl)methanamine hydrochloride 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. (2-Chloropyridin-4-yl)methanamine hydrochloride 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]. |
Name | (2-Chloropyridin-4-yl)methanamine hydrochloride |
CAS | 916210-98-5 |
Formula | C6H8Cl2N2 |
Molar Mass | 179.05 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [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. |