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NTPDase-IN-2 (compound 5g) is a selective NTPDase inhibitor with IC50s of 0.04 and 2.27 μM for h-NTPDase-2/-8, respectively. NTPDase-IN-2 non-competitively inhibits h-NTPDase-1/-2 with a Km of 74 μM for h-NTPDase-2. NTPDase-IN-2 can be used in studies of cancer, immunologic disorders as well as bacterial infections[1]. | [IC 50]
h-NTPDase-2: 0.04 μM (IC50); h-NTPDase-8: 2.27 μM (IC50); h-NTPDase-1: ＞100 μM (IC50); h-NTPDase-3: ＞100 μM (IC50) | [References]
[1] Abbas S, et al. Synthesis, characterization and biological evaluation of thiadiazole amide derivatives as nucleoside triphosphate diphosphohydrolases (NTPDases) inhibitors. Bioorg Chem. 2022 Jan;118:105456. DOI:10.1016/j.bioorg.2021.105456 |
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