Porcupine-IN-1

Modify Date: 2024-01-05 18:08:28

Porcupine-IN-1 Structure
Porcupine-IN-1 structure
Common Name Porcupine-IN-1
CAS Number 2036044-77-4 Molecular Weight 410.44
Density N/A Boiling Point N/A
Molecular Formula C25H19FN4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Porcupine-IN-1


Porcupine-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.

 Names

Name Porcupine-IN-1
Synonym More Synonyms

 Porcupine-IN-1 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

[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.

 Chemical & Physical Properties

Molecular Formula C25H19FN4O
Molecular Weight 410.44

 Synonyms

MFCD31630804
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