CD73 Inhibitor

HBM1007 is a fully human monoclonal antibody targeting CD73. HBM1007 is an extracellular enzyme expressed on the surface of stromal cells and tumor cells, capable of converting extracellular adenosine monophosphate (AMP) into adenosine, and recognizing CD73 via a unique antigenic epitope. HBM1007 inhibits both CD73-dependent and CD73-independent enzyme activities.

PSB-12379 disodium, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with K_is of 9.03 nM (rat) and 2.21 nM (human).

ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC).

2,4-Dinitrobenzenesulfonic acid (Compound 3) is a ecto-5'-Nucleotidase (CD73) inhibitor with a K_i value of 63 μM for human and 144 μM for rat. 2,4-Dinitrobenzenesulfonic acid can inhibit the hydrolysis of adenosine monophosphate (AMP) to generate adenosine. 2,4-Dinitrobenzenesulfonic acid can be used for the research of cancer.

PSB-0963 is a selective and competitive ecto-5'-nucleotidase (eN/CD73) inhibitor with a K_i of 150 nM for rat ecto-5'-nucleotidase. PSB-0963 shows high selectivity over other ectonucleotidases (NTPDases 1-3) and P2Y receptors. PSB-0963 can be used for the study of cancer.

W-GTF01 is a MGAT1 inhibitor. W-GTF01 blocks the MGAT1-catalyzed glycosylation of CD73, and inhibits CD73 dimerization, membrane translocation and adenosine production. W-GTF01 restores the function of IFNγ-producing CD8⁺ T cells, enhances tumor infiltration and activation of CD8⁺ T cells, and suppresses tumor growth. W-GTF01 can be used in research related to triple-negative breast cancer.

CD73-IN-16 (compound 18) is an inhibitor of hCD73 with IC₅₀ values of 0.28 μM.

ZM514 is a potent CD73 inhibitor with IC₅₀s of 1.39 μM and 14.65 μM for hCD73 and mCD73, respectively. ZM514 has low cytotoxicity. ZM514 can be used for researching anticancer.

Enpp-1/3-IN-1 (Compound 5j) is an ENPP1/ENPP3 inhibitor, with IC₅₀s of 0.59 μM (h-ENPP1) and 0.62 μM (h-ENPP3) respectively. Enpp-1/3-IN-1 also inhibits e5′NT (CD73) and TNAP with IC₅₀s of 0.89 μM (h-e5′NT), 5.12 μM (r-e5′NT) and 1.68 μM (h-TNAP), respectively. Enpp-1/3-IN-1 can be used for cancer research.

CD73-IN-15 (compound 12f) is a potent inhibitor of CD73, with the IC₅₀ of 60 nM. CD73-IN-15 plays an important role in cancer research.

IBI-325 is a humanized monoclonal antibody inhibitor targeting CD73. IBI-325 completely inhibits CD73 enzymatic activity without hook effect. IBI-325 reverses Adenosine monophosphate (HY-A0181)-mediated immune suppression and significantly inhibits T cell proliferation and cytokines (IL-2, IFN-γ and TNF-α) release. IBI-325 has potent antitumor activities in hPBMC-reconstituted mice model and hCD73 knock-in mice model. IBI-325 can be used for cancer immunotherapy research.

CD73-IN-12 (compound 9) is a potent inhibitor of CD73. CD73 is closely associated with tumor growth, angiogenesis and metastasis. CD73-IN-12 can be used for the study of tumor-related diseases. CD73-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

CD73-IN-18 (compound 35j) is an orally available inhibitor of extracellular 5-nucleotidase (CD73). CD73-IN-18 can be used in anti-cancer research.

S095024 is a humanized IgG1 monoclonal antibody inhibitor targeting CD73. S095024 can be used to study acute respiratory distress syndrome (ARDS), non-small cell lung cancer (NSCLC) and advanced solid tumor malignancies.

CD73/NTPDase1-IN-1 is a dual NTPDase1 and CD73 inhibitor, with IC₅₀ values of 2.20 μM and 1.70 μM against human targets, respectively. CD73/NTPDase1-IN-1 can be used in the research of diseases such as inflammation, immunity and tumors.

BK50164 is a potent CD73 inhibitor with an IC₅₀ value of 13.089 μM. BK50164 binds to CD99 with a K_D value of 1.5 μM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase.

CD73-IN-6 is a CD73 inhibitor extracted from patent WO2022007677A1 compound 2. CD73-IN-6 can be used for the research of cancer.

CD73-IN-7 (compound 13) is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-7 can be used for the study of tumor-related diseases.

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

JAB-BX102 is a human monoclonal antibody (mAb) targeting NT5E/CD73. JAB-BX102 can be used in the study of cancers such as breast cancer, pancreatic cancer, and prostate cancer.