NTPDase1

NTPDase8, encoded by ENTPD8, hydrolyzes nucleoside triphosphates and diphosphates to monophosphates, thereby shaping extracellular nucleotide availability and purinergic signaling^[1]^[2]. Mechanistically, plasma-membrane NTPDases 1, 2, 3, and 8 hydrolyze ATP and UTP in the micromolar range, but NTPDase8 differs by generating transient ADP accumulation, which may support short-lived ADP-receptor activation compared with NTPDase1^[3]. In liver, cloned human and rat NTPDase8 matched the canalicular ecto-ATPase/ATPDase, showed high bile-canalicular activity, and accounted for the major hepatic NTPDase activity^[4]. Therefore, its canalicular localization supports experimental studies of bile secretion, nucleoside salvage, and liver extracellular nucleotide metabolism^[4]. In zebrafish, entpd8 appears with distinct NTPDase-family expression profiles in brain, liver, and heart, supporting comparative models of tissue-specific nucleotide hydrolysis^[5]. In disease models, ENTPD8 was downregulated in pancreatic cancer tissues and linked to weakened CTP dephosphorylation and reduced cytidine formation^[6]. In hepatocellular carcinoma, ENTPD8 overexpression inhibited proliferation, invasion, and migration and enhanced anti-PD-L1 efficacy through miR-214-5p modulation^[7]. For inhibitor applications, sulfamoyl benzamide derivatives identified 2-chloro-5-(N-cyclopropylsulfamoyl)benzoic acid as a selective NTPDase8 inhibitor, supporting isoform-focused enzymology and purinergic-signaling assays^[8].

References:

[1]. Orlic-Milacic M, et al. Phosphate bond hydrolysis by NTPDase proteins. Reactome. 2015

[2]. Robson SC, et al. The E-NTPDase family of ectonucleotidases: Structure function relationships and pathophysiological significance. Purinergic Signal. 2006 Jun;2(2):409-30. [Content Brief]

[3]. Mateo J, et al. Functional expression of a cDNA encoding a human ecto-ATPase. Br J Pharmacol. 1999 Sep;128(2):396-402. [Content Brief]

[4]. Fausther M, et al. Cloning, purification, and identification of the liver canalicular ecto-ATPase as NTPDase8. Am J Physiol Gastrointest Liver Physiol. 2007 Mar;292(3):G785-95. [Content Brief]

[5]. Rosemberg DB, et al. NTPDase family in zebrafish: Nucleotide hydrolysis, molecular identification and gene expression profiles in brain, liver and heart. Comp Biochem Physiol B Biochem Mol Biol. 2010 Mar;155(3):230-40. [Content Brief]

[6]. An Y, et al. Identification of ENTPD8 and cytidine in pancreatic cancer by metabolomic and transcriptomic conjoint analysis. Cancer Sci. 2018 Sep;109(9):2811-2821. [Content Brief]

[7]. Zhao SQ, et al. ENTPD8 overexpression enhances anti-PD-L1 therapy in hepatocellular carcinoma via miR-214-5p inhibition. iScience. 2025 Jan 16;28(2):111819. [Content Brief]

[8]. Zaigham ZH, et al. Synthesis and biological evaluation of sulfamoyl benzamide derivatives as selective inhibitors for h-NTPDases. RSC Adv. 2023 Jul 11;13(30):20909-20915. [Content Brief]

NTPDase1 Inhibitor (1)

NTPDase1 Related Products (1):

By Type:	Pan (1)

Cat. No.	Product Name	Effect	Purity

HY-183701

CD73/NTPDase1-IN-1	Inhibitor
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.

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