PSB-12379 is an inhibitor of ecto-5’-nucleotidase (CD73; Kis = 2.21 and 9.03 nM for the recombinant human and rat enzyme, respectively).1 It is selective for CD73 over human nucleoside triphosphate diphosphohydrolase 1 (NTPDase 1), -2, and -3, ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1), -2, and -3 (Kis = >10,000 nM for all), as well as the purinergic P2Y1 and P2Y12 receptors at 10 ?M. PSB-12379 inhibits CD73 in isolated human serum with a Ki value of 18.8 nM.
1.Bhattarai, S., Freundlieb, M., Pippel, J., et al.α,β-Methylene-ADP (AOPCP) derivatives and analogues: Development of potent and selective ecto-5′-nucleotidase (CD73) inhibitorsJ. Med. Chem.586248-6263(2015)