[CAS NO. 2036044-77-4] Porcn-IN-1
PRODUCTS SPECIFICATIONS [2036044-77-4]
DESCRIPTION [2036044-77-4]
Overview
| MDL | MFCD31630804 |
|---|---|
| Molecular Weight | 410.44 |
| Molecular Formula | C25H19FN4O |
| SMILES | FC1=C(C2=CC(C)=NC=C2)N=CC(CNC(C3=CC=C(C(C=CC=C4)=C4N5)C5=C3)=O)=C1 |
Summary
Porcn-IN-1 is potent porcupine inhibitor with an IC 50 of 0.5±0.2 nM.
IC50 & 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. Porcn-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 243.64 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4364 mL | 12.1820 mL | 24.3641 mL |
| 5 mM | 0.4873 mL | 2.4364 mL | 4.8728 mL |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4364 mL |