Chemical Name: Trispiro[3H-indole-3,2'-[1,3]dioxane-2'',3'''-[3H]indole]-2,2'''(1H,1'''H)-dione
Biological ActivityInhibitor of canonical Wnt pathway signaling (IC50 = 1.17 μM); targets the β-catenin destruction complex (GSK-3β/AXIN/APC) to induce β-catenin degradation. Selective for the canonical Wnt pathway over the Sonic hedgehog (Shh) and NF-κB pathways. Blocks G1/S cell cycle progression in colorectal cancer (CRC) cell lines (GI50 = 7.8 μM).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth.
Waaler et al.
Cancer Res., 2011;71:197
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.
Shultz et al.
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