Porcn-IN-1 (Porcupine-IN-1) is an effective porcupine inhibitor (IC50: 0.5±0.2 nM).

Porcupine:0.5 Nm

Porcupine是一种酶，催化棕榈油酸添加到Wnt蛋白中的丝氨酸残基上，这一过程对于Wnt蛋白的分泌至关重要。Porcupine-IN-1在基于细胞的STheaflavin报告基因测定中与临床化合物LGK974具有相同的效力。Porcupine-IN-1强效地抑制了Wnt3A的分泌，因此被确认为Porcupine抑制剂[1]。

Porcupine-IN-1在处理人肝微粒体（57 mL/min/kg）和大鼠肝微粒体（24 mL/min/kg）时，显示出中等程度的清除率。当用小鼠微粒体（109 mL/min/kg）处理时，展现出高清除率[1]。

HEK293T cells are transfected with pLinbin-Wnt3A plasmid or vehicle control. The HEK293T cells are then treated with or without compounds (Porcupine-IN-1). Western Blot is used after 48 h to analyze both the cell lysis and culture medium[1].