| CCT 031374 hydrobromideinhibits TCF-dependent transcription, blocks BIO-induced β-catenin stabilization |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 1219184-91-4 | SDF | Download SDF |
| Chemical Name | 1-([1,1"-biphenyl]-4-yl)-2-(2H-benzo[d]imidazo[1,2-a]imidazol-9(3H)-yl)ethanone hydrobromide | ||
| Canonical SMILES | O=C(C1=CC=C(C2=CC=CC=C2)C=C1)CN3C4=CC=CC=C4N5CCN=C53.Br | ||
| Formula | C23H19N3O.HBr | M.Wt | 434.33 |
| Solubility | <21.72mg l="" in="" dmso=""> | Storage | Desiccate at RT |
| Physical Appearance | Pale yellow solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
