Porcupine-IN-1 是一种有效的Porcupine抑制剂(IC50:0.5±0.2 nM)。

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

Porcupine is an enzyme that catalyzes 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. Porcupine-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor[1].

Porcupine-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].

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].

2036044-77-4

C25H19FN4O

410.452

Porcupine-IN-1

DMSO:100 mg/mL (243.64 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years