8-BuS-AMP is a NTPDase1 inhibitor and a CD73/CD39 inhibitor, with an IC50 of 35 μM and a K i value of 0.292 μM against human NTPDase1; its K i values against human CD73 and CD39 are 1.19 μM and 0.847 μM, respectively. 8-BuS-AMP binds to the substrate-binding pockets of NTPDase1 and CD73 to effectively block the conversion of ATP and AMP to adenosine, thereby enhancing the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP possesses excellent enzymatic hydrolysis resistance and metabolic stability, resists hydrolysis by multiple NTPDase subtypes, and shows no activity against P2Y1 and P2Y12 receptors. 8-BuS-AMP can be used in purinergic signaling pathway and cancer-related studies [1] [2] [3].
In Vivo, 8-BuS-AMP (100 μM; added to histochemical reaction buffer) specifically inhibits NTPDase1-mediated ATPase activity in mouse liver vascular tissues without affecting NTPDase activity in kidney tubules[2].
In Vitro, 8-BuS-AMP (100 μM; 10 min) impairs recombinant human NTPDase1's ability to inhibit ADP-induced platelet aggregation, but does not itself induce or inhibit platelet aggregation, indicating in vitro inactivity towards platelet P2Y1 and P2Y12 receptors[2]. 8-BuS-AMP (1 μM; 0, 20, 40, 60 min) is highly metabolically stable in human and mouse liver microsomes, with half-lives of 462 min and 182 min, respectively[3]. 8-BuS-AMP (1-100 μM; 1 h) concentration-dependently inhibits nucleotide hydrolysis in human synovial fluid, reducing adenosine formation from both ε-ATP and ε-AMP[3]. 8-BuS-AMP (10-100 μM; 3 days, added daily) concentration-dependently enhances activation (via increased CD25 expression) and proliferation of human primary CD4+ and CD8+ T lymphocytes without reducing cell viability[3].
References:
[1]. Baqi Y, et al. Development of Anthraquinone Derivatives as Ectonucleoside Triphosphate Diphosphohydrolase (NTPDase) Inhibitors With Selectivity for NTPDase2 and NTPDase3. Front Pharmacol. 2020;11:1282. Published 2020 Aug 27.
[2]. Lecka J, et al. 8-BuS-ATP derivatives as specific NTPDase1 inhibitors. Br J Pharmacol. 2013;169(1):179-196.
[3]. Bi C, et al. Synthesis, Characterization, Interactions, and Immunomodulatory Function of Ectonucleotidase CD39/CD73 Inhibitor 8-Butylthioadenosine 5'-Monophosphate. ACS Pharmacol Transl Sci. 2025;8(5):1401-1415. Published 2025 Apr 3.
In Vivo, 8-BuS-AMP (100 μM; added to histochemical reaction buffer) specifically inhibits NTPDase1-mediated ATPase activity in mouse liver vascular tissues without affecting NTPDase activity in kidney tubules[2].
In Vitro, 8-BuS-AMP (100 μM; 10 min) impairs recombinant human NTPDase1's ability to inhibit ADP-induced platelet aggregation, but does not itself induce or inhibit platelet aggregation, indicating in vitro inactivity towards platelet P2Y1 and P2Y12 receptors[2]. 8-BuS-AMP (1 μM; 0, 20, 40, 60 min) is highly metabolically stable in human and mouse liver microsomes, with half-lives of 462 min and 182 min, respectively[3]. 8-BuS-AMP (1-100 μM; 1 h) concentration-dependently inhibits nucleotide hydrolysis in human synovial fluid, reducing adenosine formation from both ε-ATP and ε-AMP[3]. 8-BuS-AMP (10-100 μM; 3 days, added daily) concentration-dependently enhances activation (via increased CD25 expression) and proliferation of human primary CD4+ and CD8+ T lymphocytes without reducing cell viability[3].
References:
[1]. Baqi Y, et al. Development of Anthraquinone Derivatives as Ectonucleoside Triphosphate Diphosphohydrolase (NTPDase) Inhibitors With Selectivity for NTPDase2 and NTPDase3. Front Pharmacol. 2020;11:1282. Published 2020 Aug 27.
[2]. Lecka J, et al. 8-BuS-ATP derivatives as specific NTPDase1 inhibitors. Br J Pharmacol. 2013;169(1):179-196.
[3]. Bi C, et al. Synthesis, Characterization, Interactions, and Immunomodulatory Function of Ectonucleotidase CD39/CD73 Inhibitor 8-Butylthioadenosine 5'-Monophosphate. ACS Pharmacol Transl Sci. 2025;8(5):1401-1415. Published 2025 Apr 3.