Description
Porcupine-IN-1 is an inhibitor of the Wnt and hedgehog signaling pathways (IC
50s = 0.5 and 71 nM, respectively, in cell-based reporter assays). It inhibits secretion of Wnt3A from Wnt3A-transfected HEK293T cells when used at a concentration of 0.1 μM, indicating inhibition of porcupine, an enzyme that catalyzes palmitoylation of Wnt proteins.
Uses
Porcupine-IN-1, is a potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.
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)[1].
References
[1] ZHIXIANG XU . Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the ‘reversed’ amide scaffold[J]. Bioorganic & Medicinal Chemistry, 2016, 24 22: Pages 5861-5872. DOI:
10.1016/j.bmc.2016.09.041[2] HAIKUO MA . Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor[J]. European Journal of Medicinal Chemistry, 2018, 149: Pages 110-121. DOI:
10.1016/j.ejmech.2018.02.034
