RQ-15986

RQ-15986 is a potent and selective small molecule antagonist of the prostaglandin E2 receptor EP4 (also known as PTGER4), a G-protein-coupled receptor involved in mediating inflammation, immune modulation, and tumorigenesis. Developed originally under the code name CJ-042794, RQ-15986 has demonstrated preclinical efficacy in several models: - In oncology, it inhibits tumor growth and metastasis by blocking PGE2/EP4 signaling pathways that promote cancer cell migration, proliferation, angiogenesis (including VEGF-A/C/D production), lymphangiogenesis, and immunosuppression within the tumor microenvironment. It also prevents natural killer (NK) cell suppression by tumors[1][9]. - In inflammatory disease models such as colitis-associated colorectal cancer in rats with APC mutations, RQ-15986 reduces tumorigenesis by attenuating inflammation (suppressing cytokines like TNF-alpha and IL6), decreasing epithelial proliferation, and downregulating indoleamine 2,3-dioxygenase expression[2]. Additionally, RQ-15986 contracts the ductus arteriosus (DA) selectively in fetal rats without affecting other vessels like the aorta or marginal artery of the colon. This suggests potential utility for patent ductus arteriosus treatment with fewer side effects compared to non-selective cyclooxygenase inhibitors[1][5][6].

Other names

EP4AEP-4AEP 4A