A potent and specific small molecule inhibitor of PORCN (IC50 = 0.4 nM); greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity; orally bioavailable in mice

LGK974 – 500 µg

Brand:
Cayman
CAS:
1243244-14-5
Storage:
-20
UN-No:
Non-Hazardous - /

Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} LGK974 is a potent and specific small molecule inhibitor of PORCN (IC50 = 0.4 nM).{27368} It greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity.{27368} LGK974 is orally bioavailable in mice and induces tumor regression in mouse breast tumors produced by mammary tumor virus-driven Wnt1 signaling.{27368} It also blocks carcinogenesis in other Wnt-related tumors at doses that have limited impact on stem cell renewal.{27368,27367,21934}  

 

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Description

A potent and specific small molecule inhibitor of PORCN (IC50 = 0.4 nM); greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity; orally bioavailable in mice

Formal name: 2′,3-dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4′-bipyridine]-5-acetamide

Synonyms:  PORCN Inhibitor IV

Molecular weight: 396.4

CAS: 1243244-14-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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