CCT365623 (CCT-365623) is a potent, orally active small molecule inhibitor of lysyl oxidase (LOX) with IC50 of 0.89 uM.
CCT365623 is ∼16-fold more potent than BAPN (IC50=14.7 uM).
CCT365623 displays excellent selectivity (over 350-fold) for LOX over amine oxidase A and B (MAO-A, MAO-B) and is over 1,000-fold more selective for LOX over serum diamine oxidase.
CCT365623 inhibits LOX at ∼5 μM in MDCK cysts, whereas BAPN inhibits LOX at ∼250 μM.
CCT365623 suppresses EGFR and AKT phosphorylation driven by EGF, also inhibits HTRA1 multimer formation.
CCT365623 blocks tumour growth and metastasis in a mouse model of spontaneous breast cancer that metastasizes to the lungs.
