(D)-DT-2

(D)-DT-2 is a peptide-based, membrane-permeant and proteolytically stable inhibitor of cyclic GMP-dependent protein kinase (PKG) Iα and Iβ with nanomolar in vitro IC₅₀ values (Nickl et al. 2010, Gambaryan et al. 2011). It displays high selectivity for cyclic GMP-dependent protein kinase Iα compared to cyclic AMP-dependent protein kinase with a ratio of approximately 15,000 fold (Nickl et al. 2010). (D)-DT-2 is the newly developed D-amino acid analogue of the peptidic PKG inhibitor DT-2 (Prod. No. BLG-D051). So far, the inhibitory potential of (D)-DT-2 in in vivo applications has not been fully characterized, but seems to be variable depending on the type of biosystem used. It is recommended to control the physiological effects of (D)-DT-2 in in vivo applications by PKG specific substrate phosphorylation.