CNT2 inhibitor-1

CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.

Signaling Pathways >> Others >> Others

Research Areas >> Others

IC50: 640 nM (hCNT2)[1][2].

CNT2 inhibitor-1 (compound 48) exhibits 81-fold more potent inhibitory activity than the parent compound 12. In addition, CNT2 inhibitor-1 exhibits inhibitory activity 1500-fold more potent than that of 2’-deoxy-5-fluorouridine, phlorizin, and 7,8,3’-trihydroxyflavone, which are well-known hCNT2 inhibitors[1]. CNT2 inhibitor-1 (compound 1) is a potent inhibitor with poor solubility[2].

[1]. Tatani K, et al. Identification of 8-aminoadenosine derivatives as a new class of human concentrative nucleoside transporter 2 inhibitors. ACS Med Chem Lett. 2015 Jan 28;6(3):244-8.

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