1H-Indole-6-carbonitrile, 3-[5-bromo-6-[[(2R,3R)-2-(4-fluorophenyl)-3-(hydroxymethyl)-4-morpholinyl]carbonyl]-1-methyl-1H-benzimidazol-2-yl]-1-ethyl-, rel-

PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity[1]. PDE12-IN-1 inhibits the EMCV-induced cytopathic effect in HeLa Ohio cells with a pIC50 of 6.7. PDE12-IN-1 inhibits HeLa Ohio cell proliferation in the absence of EMCV infection with a pIC50 of 5.7. PDE12-IN-1 inhibits the proliferation of both HeLa and HeLaδPDE12 cells with a pIC50 of 5.7. PDE12-IN-1 inhibits HRV infection with a pIC50 of 6.9[1].

[1]. Wood ER, et al. The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors. J Biol Chem. 2015 Aug 7;290(32):19681-96.