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Wnt-C59
Cat No.
CEI-1582
Description
Wnt-C59 (C59) is an inhibitorof PORCN for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM.
Product Overview
Wnt-C59 is a selective inhibitor of Wnt signaling with IC50 value of 74 pM. 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. 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. 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. 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. 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.
CAS No.
1243243-89-1
Molecular Weight
379.45
Purity
0.9992
Storage
Store at-20°C
Targets
PORCN
IC50
74 pM
Molecular Formula
C25H21N3O
Chemical Name
2-[4-(2-methylpyridin-4-yl)phenyl]-N-(4-pyridin-3-ylphenyl)acetamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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