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)
体外研究
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.
体内研究
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).
分子式
C25H19FN4O
分子量
410.44
CAS号
2036044-77-4
运输条件
Room temperature in continental US; may vary elsewhere.