CCT 031374 hydrobromide |
| カタログ番号GC10253 |
CCT 031374 臭化水素酸塩は、β-カテニン/転写因子 (TCF) 複合体シグナル伝達の強力な阻害剤です。 CCT031374 は、Wnt シグナル伝達経路の遺伝子の TCF 依存性転写を阻害します。 CCT 031374 には抗腫瘍活性があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1219184-91-4
Sample solution is provided at 25 µL, 10mM.
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CCT 031374 hydrobromide is a selective inhibitor of Wnt/β-catenin signaling pathway [1].
The Wnt/β-catenin pathway is activated by the binding of Wnt ligand to a complex comprising LRP5/6 and Frizzled (Fz) receptors and then activates transcription factor/β-catenin-dependent transcription [1].
CCT 031374 hydrobromide is a selective Wnt/β-catenin signaling pathway inhibitor. CCT031374 inhibited BIO-induced β-catenin accumulation in L-cells with IC50 value of 6.1 μM. In HCT116 human colon cancer cell line, CCT031374 inhibited cell proliferation by inducing apoptosis. In mouse L-cells, BIO, a GSK-3 inhibitor, significantly increased total β-catenin levels. While CCT031374 inhibited BIO-induced accumulation of β-catenin in both nuclear and cytosolic. In U2OS GFP-β-catenin human osteosarcoma cells, CCT031374 induced the formation of GFP-β-catenin aggregates. In human neurogenic embryoid bodies, CCT031374 reduced the mRNA levels of endogenous LEF1. Also, CCT031374 inhibited cell growth with GI values of 11.5, 13.9, 13.2, 9.6 and 44 μM in HT29, HCT116, SW480, SNU475 and CCD841Co cancer cell lines, respectively [1].
Reference:
[1]. Ewan K, Pajak B, Stubbs M, et al. A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription. Cancer Res, 2010, 70(14): 5963-5973.
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