8-Cl-cAMP is a potent stimulator of cAMP-dependent protein kinases with high affinity for sites A and B of PKA type I. in addition it shows high site selectivity for site B of PKA type II. The analogue is degraded by cyclic nucleotide phosphodiesterases more slowly compared to natural cyclic AMP.
The increased lipophilicity which resembles 8-bromo cyclic AMP and Sp-cAMPS enables membrane permeability in several biosystems.
Due to its ability to stop growth of several cancer cell lines at very low doses, its therapeutic use is under investigation. However, recent reports on active 8-Cl- metabolites showed that also degradation products could be responsible for cytostatic properties.
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