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Submit ReviewICG 001
Description: Inhibits TCF/β-catenin-mediated transcription
Chemical Name: (6S,9aS)-Hexahydro-6-[(4-hydroxyphenyl)methyl]-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for ICG 001
ICG 001 is an inhibitor of TCF/β-catenin-mediated transcription. Selectively inhibits β-catenin/CBP interaction; displays no effect on β-catenin/p300 interaction. Exhibits growth inhibitory effects in colon carcinoma cell lines (SW480 and HCT-116 cells); also displays efficacy in Min mouse and nude mouse SW620 xenograft models.
Technical Data for ICG 001
| M. Wt | 548.63 |
| Formula | C33H32N4O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 780757-88-2 |
| PubChem ID | 11238147 |
| InChI Key | HQWTUOLCGKIECB-XZWHSSHBSA-N |
| Smiles | O=C1CCN(C(NCC5=CC=CC=C5)=O)[C@]2([H])N1[C@@H](CC6=CC=C(O)C=C6)C(N(CC3=C(C=CC=C4)C4=CC=C3)C2)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ICG 001
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.86 | 100 | |
| ethanol | 27.43 | 50 |
Preparing Stock Solutions for ICG 001
The following data is based on the product molecular weight 548.63. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.82 mL | 9.11 mL | 18.23 mL |
| 5 mM | 0.36 mL | 1.82 mL | 3.65 mL |
| 10 mM | 0.18 mL | 0.91 mL | 1.82 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets for ICG 001
References for ICG 001
References are publications that support the biological activity of the product.
Emami et al (2004) A small molecule inhibitor of β-catenin/CREB-binding protein transcription. Proc.Natl.Acad.Sci.USA 101 12682 PMID: 15314234
De Sousa et al (2011) Targeting wnt signaling in colon cancer stem cells. Clin.Cancer Res. 17 647 PMID: 21159886
Zhou et al (2012) Interactions between β-catenin and transforming growth factor-β signaling pathways mediate epithelial-mesenchymal transition and are dependent on the transcriptional co-activator cAMP-respo J.Biol.Chem. 287 7026 PMID: 22241478
If you know of a relevant reference for ICG 001, please let us know.
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Keywords: ICG 001, ICG 001 supplier, ICG001, inhibits, inhibitors, TCF, t, cell, factors, b-catenin, beta-catenin, β-catenin, signaling, signalling, selectively, 847591-62-2, Beta-catenin, 4505, Tocris Bioscience
16 Citations for ICG 001
Citations are publications that use Tocris products. Selected citations for ICG 001 include:
Nishiya et al (2014) A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway. Chem Biol 21 530 PMID: 24684907
Rothberg (2018) Mtf2-PRC2 control of canonical Wnt signaling is required for definitive erythropoiesis. Cell Discov 4 21 PMID: 29736258
Koopmans et al (2017) β-Catenin Directs Nuclear Factor-κB p65 Output via CREB-Binding Protein/p300 in Human Airway Smooth Muscle. Front Immunol 8 1086 PMID: 28943877
Preethi et al (2020) High-Throughput Drug Screening Identifies a Potent Wnt Inhibitor that Promotes Airway Basal Stem Cell Homeostasis. Cell Rep 30 2055-2064.e5 PMID: 32075752
Kling et al (2018) Temporal Regulation of Natural Killer T Cell Interferon Gamma Responses by β-Catenin-Dependent and -Independent Wnt Signaling. Front Immunol 9 483 PMID: 29616022
Long et al (2016) Integrin signalling regulates the expansion of neuroepithelial progenitors and neurogenesis via Wnt7a and Decorin. J Clin Invest 7 10354 PMID: 26838601
Gravesen (2018) Effect of inhibition of CBP-coactivated β-catenin-mediated Wnt signalling in uremic rats with vascular calcifications. PLoS One 13 e0201936 PMID: 30075015
Koopmans et al (2016) Selective targeting of CREB-binding protein/β-catenin inhibits growth of and extracellular matrix remodelling by airway smooth muscle. Br J Pharmacol 173 3327 PMID: 27629364
Laurent et al (2021) Network-Based Integration of Multi-Omics Data Identifies the Determinants of miR-491-5p Effects. Cancers (Basel) 13 PMID: 34439123
Linh et al (2021) Loss of BAF Complex in Developing Cortex Perturbs Radial Neuronal Migration in a WNT Signaling-Dependent Manner. Front Mol Neurosci 14 687581 PMID: 34220450
Heinrich et al (2017) WNT ligands contribute to the immune response during septic shock and amplify endotoxemia-driven inflammation in mice. Blood Adv 1 1274-1286 PMID: 29296769
Benoit et al (2017) Sam68 Allows Selective Targeting of Human Cancer Stem Cells. Cell Chem Biol 24 833 PMID: 28648376
Zinecker et al (2017) ICG-001 affects DRP1 activity and ER stress correlative with its anti-proliferative effect. Oncotarget 8 106764 PMID: 29290987
Gu et al (2017) Titanium particle-induced osteogenic inhibition and bone destruction are mediated by the GSK-3β/β-catenin signal pathway. Cell Death Dis 8 e2878 PMID: 28617442
Boulter et al (2015) WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. PLoS One 125 1269 PMID: 25689248
Corbett et al (2015) Non-Canonical Wnt Predominates in Activated Rat Hepatic Stellate Cells, Influencing HSC Survival and Paracrine Stimulation of Kupffer Cells. J Immunol 10 e0142794 PMID: 26566235
Do you know of a great paper that uses ICG 001 from Tocris? Please let us know.
Reviews for ICG 001
Average Rating: 5 (Based on 1 Review.)
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Good product..
By
Anonymous on 07/07/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: BLaER1 DRP1 KO cell lines
BLaER1 DRP1 KO cell lines C12 and F11 and a corresponding wt-control cell line were treated with 10 µM ICG-001 or vehicle control for 2.5 h.
Literature in this Area
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Pathways for ICG 001
