Porcupine-IN-1
Names
Biological Activity
[Description]:
Porcupine-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.
[Related Catalog]:
[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. Porcupine-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor[1].
[In Vivo]
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].
[Cell Assay]
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].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C25H19FN4O
[ Molecular Weight ]:
410.44