cd73 in 5

CD73-IN-5 is a highly potent and selective small molecule inhibitor of CD73, demonstrating non-nucleotide characteristics. It exerts its inhibitory effects with a remarkable IC50 value of 19 nM.

CD73-IN-18 (compound 35j) is an orally effective inhibitor of the extracellular 5'-nucleotidase (CD73) enzyme. It can be utilized in anticancer research.

PSB-24000 (Compound 27) is a selective ecto-5'-nucleotidase (CD73) inhibitor with a Ki value of 563 nM for inhibiting human CD73, and a Ki of 481 nM in membrane-bound CD73 in triple-negative breast cancer cells. It disrupts CD73’s recognition and action on substrate AMP, preventing AMP-induced immunosuppressive and pro-cancer adenosine production. PSB-24000 is promising for cancer research.

PD-L1/CD-73-IN-1 (compound CC-5) is an inhibitor of PD-L1 and CD73, with IC50 values of 6 nM and 0.773 μM, respectively. It effectively inhibits tumor cell growth both in vitro and in vivo.

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.

CD73-IN-21 (Compound 12f) is an inhibitor of ecto-5′-nucleotidase (CD73), with Ki values of 20 nM for hCD73 and 302 nM for mCD73. It is applicable in research related to cancers, such as breast cancer.

2,4-Dinitrobenzenesulfonic acid (Compound 3) is an extracellular 5'-nucleotidase (CD73) inhibitor, with a Ki value of 63 μM for human and 144 μM for rat. It inhibits the hydrolysis of adenosine monophosphate (AMP) to adenosine and 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)

CD73-IN-7 is a potent CD73 inhibitor used for preparing medications for tumor-related diseases. CD73 catalyzes the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), inducing immunosuppressive effects and promoting tumor proliferation and/or metastasis [1].

CD73-IN-9, a potent CD73 inhibitor, is used in preparing medication for tumor-related diseases. CD73 catalyzes the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), which can induce immunosuppressive effects and promote tumor proliferation and/or metastasis [1].

CD73-IN-10 can be used in preparing tumor-related diseases medicament. CD73-IN-10 is a potent CD73 inhibitor that can catalyze the adenosine production from extracellular 5'-phosphate adenosine (5'-AMP). Adenosine induces immunosuppression and can promote tumor proliferation and/or metastasis [1].

CD73-IN-11 is able to used for tumor-related diseases medicament preparing. CD73-IN-11 is an effective CD73 inhibitor. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP) which induce immunosuppression and promote tumor proliferation and/or metastasis [1].

CD73-IN-8, a potent CD73 inhibitor, prevents the catalytic activity of CD73, an enzyme responsible for converting extracellular 5'-phosphate adenosine (5'-AMP) to adenosine. Adenosine, once produced, can induce immunosuppressive effects and facilitate tumor proliferation and/or metastasis. Therefore, CD73-IN-8 holds promise in the development of therapeutic interventions for tumor-related diseases[1].

PSB-12379 disodium is a nucleotide analogue acting as a potent inhibitor of Ecto-5'-Nucleotidase (CD73), demonstrating inhibitory constants (Ki) of 9.03 nM in rats and 2.21 nM in humans [1] [2].

Uliledlimab is a humanized monoclonal antibody with potent inhibitory activity against CD73, the ecto-5'-nucleotidase enzyme that catalyzes the conversion of extracellular AMP to adenosine. Uliledlimab reduces extracellular adenosine production, thereby modulating immunosuppressive pathways. Uliledlimab holds significant potential for use in immuno-oncology and cancer research.

CD73-IN-4 is a potent and selective methylenephosphonic acid CD73 inhibitor.

Ucenprubart (NZV930) is a high-affinity humanized monoclonal antibody that specifically targets CD73 (ecto-5'-nucleotidase). By inhibiting the enzymatic activity of CD73, Ucenprubart prevents the conversion of extracellular AMP into the immunosuppressive metabolite adenosine, thereby relieving immunosuppression in the tumor microenvironment and promoting antitumor immunity. It is widely investigated in cancer immunotherapy research.