For research use only. Not for therapeutic Use.
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].
| Catalog Number | I015554 |
| CAS Number | 2259620-80-7 |
| Synonyms | 3-[5-bromo-6-[(2R,3R)-2-(4-fluorophenyl)-3-(hydroxymethyl)morpholine-4-carbonyl]-1-methylbenzimidazol-2-yl]-1-ethylindole-6-carbonitrile |
| Molecular Formula | C31H27BrFN5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C31H27BrFN5O3/c1-3-37-16-23(21-9-4-18(15-34)12-26(21)37)30-35-25-14-24(32)22(13-27(25)36(30)2)31(40)38-10-11-41-29(28(38)17-39)19-5-7-20(33)8-6-19/h4-9,12-14,16,28-29,39H,3,10-11,17H2,1-2H3/t28-,29-/m1/s1 |
| InChIKey | YWMAQKQMUXYMAZ-FQLXRVMXSA-N |
| SMILES | CCN1C=C(C2=C1C=C(C=C2)C#N)C3=NC4=C(N3C)C=C(C(=C4)Br)C(=O)N5CCOC(C5CO)C6=CC=C(C=C6)F |
| Reference | [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. |
