Porcn-IN-1

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

Product information

CAS Number: 2036044-77-4

Molecular Weight: 410.44

Formula: C25H19FN4O

Chemical Name: N-((3-fluoro-2'-methyl-2, 4'-bipyridin-5-yl)methyl)-9H-carbazole-2-carboxamide

Smiles: CC1=CC(=CC=N1)C1=NC=C(CNC(=O)C2=CC=C3C(=C2)NC2=CC=CC=C32)C=C1F

InChiKey: GOMFFTZBKYVUOE-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (243.64 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. Porcn-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor.

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).

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.

Products are for research use only. Not for human use.