Mozavaptan is an orally bioavailable antagonist of vasopressin V2 receptors (Ki = 9.42 nM in HeLa cells expressing the human receptor). It is selective for vasopressin V2 over V1 receptors (IC50s = 14 and 1,200 nM, respectively) in radioligand binding assays using rat kidney and rat liver membranes that endogenously...

5-Azacytidine, a chemical analogue of the DNA and RNA nucleoside cytidine, is an inhibitor of DNA methyltransferases, potentially serving to reverse epigenetic changes. It reduces hypermethylation associated with certain diseases, including myelodysplastic syndromes (IC50s = 2.4 and 2.6 µM for in vitro anti-myeloma...

Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins. This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer. Wnt-C59 is a potent inhibitor of PORCN, as measured by prevention of Wnt3A...

Forskolin (Cay-11018) is a naturally-occurring diterpene that activates adenylyl cyclase through its catalytic subunit and is commonly used to raise levels of cAMP in a wide variety of intact cells and tissue preparations. 1,9-dideoxy Forskolin is an analog of forskolin that interacts with, but does not activate,...