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Apexbio Technology LLC LGK-974 1243244-14-5 50mg
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Supplier:  Apexbio Technology LLC B230750

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LGK-974 (CAS 1243244-14-5) is a small molecule inhibitor specifically targeting Porcupine (PORCN) an enzyme essential for the secretion and activity of Wnt proteins LGK-974 inhibits PORCN with an IC50 of approximately 1 nM thus suppressing Wnt signaling pathways as evidenced by dose-dependent reduction in Wnt secretion and downstream AXIN2 expression In cellular assays LGK-974 demonstrated negligible cytotoxicity even at 20 M Animal model studies including MMTV-Wnt1-driven tumors and human head and neck squamous carcinoma (HNSCC) xenografts indicate LGK-974 reduces tumor growth and decreases phosphorylation of LRP6 LGK-974 is thus valuable for investigating PORCN-mediated Wnt signaling and associated cancers

Catalog No. 50-000-63468


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