CCT 031374 hydrobromideInhibits TCF-dependent transcription CAS# 1219184-91-4 |
- CCG-63802
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| Cas No. | 1219184-91-4 | SDF | Download SDF |
| PubChem ID | 18554738 | Appearance | Powder |
| Formula | C23H20BrN3O | M.Wt | 434.33 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO | ||
| Chemical Name | 2-(1,2-dihydroimidazo[1,2-a]benzimidazol-4-yl)-1-(4-phenylphenyl)ethanone;hydrobromide | ||
| SMILES | C1CN2C3=CC=CC=C3N(C2=N1)CC(=O)C4=CC=C(C=C4)C5=CC=CC=C5.Br | ||
| Standard InChIKey | MPILENOYNNNGKO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H19N3O.BrH/c27-22(19-12-10-18(11-13-19)17-6-2-1-3-7-17)16-26-21-9-5-4-8-20(21)25-15-14-24-23(25)26;/h1-13H,14-16H2;1H | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Inhibitor of TCF-dependent transcription. Blocks BIO-induced β-catenin stabilization; reduces nuclear and cytosolic β-catenin levels in mouse L-cells. Inhibits growth and reduces TCF-dependent transcription in SW480 colon carcinoma cells. |
CCT 031374 hydrobromide Dilution Calculator
CCT 031374 hydrobromide Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3024 mL | 11.512 mL | 23.024 mL | 46.0479 mL | 57.5599 mL |
| 5 mM | 0.4605 mL | 2.3024 mL | 4.6048 mL | 9.2096 mL | 11.512 mL |
| 10 mM | 0.2302 mL | 1.1512 mL | 2.3024 mL | 4.6048 mL | 5.756 mL |
| 50 mM | 0.046 mL | 0.2302 mL | 0.4605 mL | 0.921 mL | 1.1512 mL |
| 100 mM | 0.023 mL | 0.1151 mL | 0.2302 mL | 0.4605 mL | 0.5756 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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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A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription.[Pubmed:20610623]
Cancer Res. 2010 Jul 15;70(14):5963-73.
The Wnt signaling pathway is frequently deregulated in cancer due to mutations in genes encoding APC, beta-catenin, and axin. To identify small-molecule inhibitors of Wnt signaling as potential therapeutics, a diverse chemical library was screened using a transcription factor reporter cell line in which the activity of the pathway was induced at the level of Disheveled protein. A series of deconvolution studies was used to focus on three compound series that selectively killed cancer cell lines with constitutive Wnt signaling. Activities of the compounds included the ability to induce degradation of beta-catenin that had been stabilized by a glycogen synthase kinase-3 (GSK-3) inhibitor. This screen illustrates a practical approach to identify small-molecule inhibitors of Wnt signaling that can seed the development of agents suitable to treat patients with Wnt-dependent tumors.
