Description
SQ 22,536 is an inhibitor of adenylyl cyclase with an IC
50 value of 13 μM for inhibition of prostaglandin E
1-
stimulated increase in cAMP in intact platelets. It has been used to evaluate adenylyl cyclase activity during iloprost-
induced vasorelaxation of isolated pulmonary veins or aorta in several research paradigms, inhibiting cAMP elevation at concentrations of 100-
300 μM without effecting relaxation.
Uses
SQ 22,536 was used to study the role of adenylate cyclase in differentiation of PC12 cells and in gap junctional intercellular communication in breast cancer cells.
Definition
ChEBI: A nucleoside analogue that is adenine in which the nitrogen at position 9 has been substituted by a tetrahydrofuran-2-yl group. It is an adenylate cyclase inhibitor.
Biological Activity
Inhibitor of adenylyl cyclase (IC 50 = 1.4 μ M). Inhibits PGE 1 -stimulated increases in cAMP levels in intact human platelets.
Biochem/physiol Actions
SQ 22,536 is an effective inhibitor of not only basal but also prosptaglandin E1-activated adenylate cyclase activities in platelets.1 It reverses hyperalgesia contralaterally and ipsilaterally when injected intramuscularly in rats.2
