Wnt-C59

Wnt-C59

Catalog Number:
L002369688APE
Mfr. No.:
APE-A8685
Price:
$349
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          2-[4-(2-methylpyridin-4-yl)phenyl]-N-(4-pyridin-3-ylphenyl)acetamide
          CAS Number
          1243243-89-1
          Molecular Formula
          C25H21N3O
          Molecular Weight
          379.45
          Appearance
          A solid
          Purity
          99.92%
          Solubility
          insoluble in H2O; ≥18,.95 mg/mL in DMSO; ≥9.47 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Zhang J, Cai H, et al. "LGR5, a novel functional glioma stem cell marker, promotes EMT by activating the Wnt/β-catenin pathway and predicts poor survival of glioma patients." J Exp Clin Cancer Res.2018 Sep 12;37(1):225. PMID:30208924
          2. Cantwell MT, Farrar JS, et al. "STAT3 suppresses Wnt/β-catenin signaling during the induction phase of primary Myf5+ rown dipogenesis." Cytokine. 2018 Jun 19. pii: S1043-4666(18)30222-9. PMID:29934048

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