Name | Porcupine-IN-1 |
Synonyms | CS-2802 PORCN-IN-1 Porcupine-IN-1 Porcn inhibitor 1 Porcupine-IN-1 free base 9H-Carbazole-2-carboxamide, N-[(3-fluoro-2'-methyl[2,4'-bipyridin]-5-yl)methyl]- |
CAS | 2036044-77-4 |
Molecular Formula | C25H19FN4O |
Molar Mass | 410.44 |
Storage Condition | 2-8℃ |
MDL | MFCD31630804 |
In vitro study | 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. |
In vivo study | 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). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.436 ml | 12.182 ml | 24.364 ml |
5 mM | 0.487 ml | 2.436 ml | 4.873 ml |
10 mM | 0.244 ml | 1.218 ml | 2.436 ml |
5 mM | 0.049 ml | 0.244 ml | 0.487 ml |
biological activity | Porcn-IN-1 are effective porcupine inhibitors with an IC50 value of 0.5±0.2 nM. |
target | IC50: 0.5±0.2 nM (Porcupine inhibitor) |