Porcn-IN-1

2036044-77-4

C25H19FN4O

DMSO : >= 100 mg/mL (243.64 mM)

Stem Cell/Wnt

Porcn-IN-1 is potent porcupine inhibitor with an IC₅₀ of 0.5+/-0.2 nM. IC50 & Target: IC50: 0.5+/-0.2 nM (Porcupine inhibitor)^[1] In Vitro: Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, a process which is required for the secretion of Wnt proteins. Porcupine-IN-1 is as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Porcn-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor^[1]. In Vivo: Porcn-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg). It exhibits high clearance when treated with mouse microsomes (109 mL/min/kg)^[1].