cd73 in 3

CD73-IN-3 (LY-3475070) 是一种有效的选择性 CD73 抑制剂，IC50 为 28 nM，具有癌症的研究潜力。

PSB-0963 是一种选择性竞争性胞外-5'-核苷酸酶 (eN/CD73) 抑制剂，其对大鼠胞外-5'-核苷酸酶的Ki值为150 nM。与其他胞外核苷酸酶 (NTPDases 1-3) 和 P2Y 受体相比，PSB-0963 显示出更高的选择性，适用于癌症研究。

Enpp-1/3-IN-1 (Compound 5j) 是一种ENPP1/ENPP3抑制剂，其IC50分别为0.59 μM (h-ENPP1)和0.62 μM (h-ENPP3)。此外，Enpp-1/3-IN-1 还能够抑制 e5′NT (CD73)和TNAP，其IC50值为0.89 μM (h-e5′NT)、5.12 μM (r-e5′NT)和1.68 μM (h-TNAP)。该化合物可应用于癌症研究。

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)