For research use only. Not for therapeutic Use.
Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.
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[1].
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].
| Catalog Number | I014458 |
| CAS Number | 2036044-77-4 |
| Synonyms | N-[[5-fluoro-6-(2-methylpyridin-4-yl)pyridin-3-yl]methyl]-9H-carbazole-2-carboxamide |
| Molecular Formula | C25H19FN4O |
| Purity | ≥95% |
| InChI | InChI=1S/C25H19FN4O/c1-15-10-17(8-9-27-15)24-21(26)11-16(13-28-24)14-29-25(31)18-6-7-20-19-4-2-3-5-22(19)30-23(20)12-18/h2-13,30H,14H2,1H3,(H,29,31) |
| InChIKey | GOMFFTZBKYVUOE-UHFFFAOYSA-N |
| SMILES | CC1=NC=CC(=C1)C2=C(C=C(C=N2)CNC(=O)C3=CC4=C(C=C3)C5=CC=CC=C5N4)F |
| Reference | [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. |
