Porcupine-Inhibitors-Modulators-生命科学试剂-MedChemExpress.pdf

Porcupine   Porcupine (Porc) protein may be involved in secretion or ER transport, as Wingless is retained in the ER in porcupine mutant Drosophila embryos. In C. elegans, the porcupine homolog mom-1 has a similar function in promoting secretion of the Wnt protein Mom-2. Porcupine has some homology to a family of o-acyl transferases and may be involved in lipid modification of Wnt proteins. A special form of monounsaturated palmitoylation has been detected on a serine residue in the Wnt protein and could be mediated by porc as well. The human Porcupine gene is implicated in a genetic disease, Focal dermal hypoplasia. Porcupine, encodes a multipass transmembrane ER protein, which is required for normal distribution of Wg in embryos. Porc stimulates the processing of Wg when expressed in Drosophila cells in vitro and is also necessary for the localization of Drosophila Wnt-3 on the axon tracts of the embryonic central nervous system. www.MedChemE 1 Porcupine Inhibitors ETC-159 GNF-6231 (ETC-1922159) Cat. No.: HY-18988 Cat. No.: HY-100408 ETC-159 (ETC-1922159) is a potent, orally GNF-6231 is a potent, selective, and orally available PORCN inhibitor. ETC-159 inhibits bioavailable Porcupine inhibitor that blocks Wnt β-catenin reporter activity with an IC50 of 2.9 signaling. 1) GNF-6231 shows IC50s of greater than nM. 10 μM on all CYP isoforms tested 2) GNF-6231 have