(2-Chloropyridin-4-yl)methanamine hydrochloride

• CAT Number: I013077
• CAS Number: 916210-98-5
• Molecular Formula: C6H8Cl2N2
• Molecular Weight: 179.05
• Purity: ≥95%
• Synonyms: (2-chloropyridin-4-yl)methanamine;hydrochloride
• InChI: InChI=1S/C6H7ClN2.ClH/c7-6-3-5(4-8)1-2-9-6;/h1-3H,4,8H2;1H
• InChIKey: BWSUKLOBJGMGCJ-UHFFFAOYSA-N
• SMILES: C1=CN=C(C=C1CN)Cl.Cl

(2-Chloropyridin-4-yl)methanamine hydrochloride is a selective LOXL2 inhibitor with an IC50 of 126 nM.
(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].

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.
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