ATI-2341

Description: ATI-2341, a pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is a novel and selective allosteric agonist that activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 could inhibit NKH477-induced cAMP accumulation in CXCR4-HEK cells dose-dependently, but showed no effect in naive HEK-293 parental cells. Pretreatment of CXCR4- HEK cells with pertussis toxin completely abrogated the ability of ATI-2341 to inhibit cAMP accumulation. ATI-2341 could also induce a dose-dependent increase in intracellular calcium in cells transfected with wild-type CXCR4 whereas having no effect on untransfected cells.

References: Proc Natl Acad Sci U S A. 2010 Dec 21; 107(51):22255-9.