1802226-78-3

PSB-12379 is an inhibitor of ecto-5’-nucleotidase (CD73; K_is = 2.21 and 9.03 nM for the recombinant human and rat enzyme, respectively). 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 (K_is = >10,000 nM for all), as well as the purinergic P2Y₁ and P2Y₁₂ receptors at 10 μM. PSB-12379 inhibits CD73 in isolated human serum with a K_i value of 18.8 nM.

PSB-12379, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human)[1][2].

[1] Bhattarai S, et al. α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5'-Nucleotidase (CD73) Inhibitors. J Med Chem. 2015 Aug 13;58(15):6248-63. DOI:10.1021/acs.jmedchem.5b00802
[2] X-Ray Co-Crystal Structure Guides the Way to Subnanomolar Competitive Ecto-5 -Nucleotidase (CD73) Inhibitors for Cancer Immunotherapy Sanjay Bhattarai. Adv. Therap. 2019, 2, 1900075.