Bioactivity | Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11. |
CAS | 185246-32-6 |
Formula | C18H14BrN5NaO6PS |
Molar Mass | 562.27 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Jäger, et al. Activation of PDE10 and PDE11 phosphodiesterases. J. Biol. Chem. 287(2), 1210-1219 (2012). |