Porcn-IN-1 is potent porcupine inhibitor with an IC 50 of 0.5±0.2 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 0.5±0.2 nM (Porcupine inhibitor)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Xu Z, et al. Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the reversed amide scaffold.