cd73 in 3

CD73-IN-3 (LY-3475070) is a potent and selective CD73 inhibitor with an IC50 of 28 nM, and its use alone or in combination with pembrolizumab is currently being tested in patients with advanced cancer.

PSB-0963 is a selective competitive extracellular 5'-nucleotidase (eN/CD73) inhibitor with a Ki value of 150 nM for rat extracellular 5'-nucleotidase. It exhibits greater selectivity compared to other extracellular nucleotidases (NTPDases 1-3) and P2Y receptors. PSB-0963 is applicable in cancer research.

Enpp-1/3-IN-1 (Compound 5j) serves as an inhibitor for ENPP1 and ENPP3, with IC50 values of 0.59 μM for h-ENPP1 and 0.62 μM for h-ENPP3, respectively. This compound also inhibits e5′NT (CD73) and TNAP, exhibiting IC50 values of 0.89 μM for h-e5′NT, 5.12 μM for r-e5′NT, and 1.68 μM for h-TNAP. Enpp-1/3-IN-1 is applicable in cancer research.

Adenosine 5'-methylenediphosphate is an inhibitor of ecto-5'-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5'-monophosphate , adenosine 5'-diphosphate , or adenosine 5'-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5'-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg/mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase/CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto\5′\nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)