Porcupine-IN-1( Porcupine-IN-1 | MDK-4774 | MDK 4774 | MDK4774 )

Catalog No. M18214 CAS No. 2036044-77-4

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

Porcupine-IN-1
Note

Research use only, not for human use.
Brief Description

Porcupine-IN-1 is an effective porcupine inhibitor (IC50: 0.5±0.2 nM).
Description

MDK-4774, Porcupine-IN-1, is a Porcupine inhibitor.
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).
Synonyms

Porcupine-IN-1 | MDK-4774 | MDK 4774 | MDK4774
Pathway

Others
Target

Other Targets
Recptor

Porcupine
Research Area

Cancer
Indication

——

CAS Number

2036044-77-4
Formula Weight

410.44
Molecular Formula

C25H19FN4O
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 100 mg/mL; 243.64 mM
SMILES

Cc1cc(ccn1)-c1ncc(CNC(=O)c2ccc3c(c2)[nH]c2ccccc32)cc1F
Chemical Name

N-((3-Fluoro-2’-methyl[2,4’-bipyridin]-5-yl)methyl)-9H-carbazole-2-carboxamide

1.Xu Z, Xu X, O’Laoi R, et al. Bioorganic & medicinal chemistry, 2016, 24(22): 5861-5872.

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