Wnt-C59 (Synonyms: PORCN Inhibitor II) |
Catalog No.GC13658 |
Wnt-C59(C59)는 IC50이 74pM인 매우 강력한 경구 고슴도치(PORCN) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1243243-89-1
Sample solution is provided at 25 µL, 10mM.
Wnt-C59 is a selective inhibitor of Wnt signaling with IC50 value of 74 pM [1].
Wnt signaling pathways are a group of signal transduction pathways made of proteins and play an important role in passing signals from outside of a cell through cell surface receptors to the inside of the cell [1, 2].
Wnt-C59 is a potent Wnt inhibitor and has a different selectivity with the reported Wnt inhibitor crizotinib. When tested with HT1080 and Hela cells, Wnt-C59 showed inhibition on activation of a multimerized TCF-binding site driving luciferase mediated by Wnt3A by completely abrogating Wnt secretion [1]. In 5 human CC cell lines CC-LP-1, SUN-1079, WITT-1, SNU-1196, and CC-SW-1, Wnt-C59 treatment decreased cell viability, reduced cell proliferation and increased cell apoptosis by inhibiting Wnt signaling [2].
In C57/BL6 mice model transplanted with fragments from 2 independent primary MMTV-WNT1 tumors, oral administration of Wnt-C59 (10 mg/kg/d) for 17 days significantly arrested tumor growth and decreased tumor weights after sacrificing mice [1]. When tested with CD1 nude mice model with CC cell lines (CC-LP-1 and CC-SW-1) subcutaneous xenograft into the flanks, administration ofWnt-C59 inhibited cell growth and increased cell apoptosis compared with control group [2].
References:
[1]. Proffitt, K.D., et al., Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res, 2013. 73(2): p. 502-7.
[2]. Boulter, L., et al., WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. J Clin Invest, 2015. 125(3): p. 1269-85.
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