ICG 001
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%
Biological Activity
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
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.
Background References
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Targeting wnt signaling in colon cancer stem cells.
De Sousa et al.
Clin.Cancer Res., 2011;17:647 -
A small molecule inhibitor of β-catenin/CREB-binding protein transcription.
Emami et al.
Proc.Natl.Acad.Sci.USA, 2004;101:12682 -
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
Zhou et al.
J.Biol.Chem., 2012;287:7026
Product Datasheets
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Citations for ICG 001
The citations listed below are publications that use Tocris products. Selected citations for ICG 001 include:
16 Citations: Showing 1 - 10
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Loss of BAF Complex in Developing Cortex Perturbs Radial Neuronal Migration in a WNT Signaling-Dependent Manner.
Authors: Linh Et al.
Front Mol Neurosci 2021;14:687581
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Network-Based Integration of Multi-Omics Data Identifies the Determinants of miR-491-5p Effects.
Authors: Laurent Et al.
Cancers (Basel) 2021;13
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High-Throughput Drug Screening Identifies a Potent Wnt Inhibitor that Promotes Airway Basal Stem Cell Homeostasis.
Authors: Preethi Et al.
Cell Rep 2020;30:2055-2064.e5
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Temporal Regulation of Natural Killer T Cell Interferon Gamma Responses by β-Catenin-Dependent and -Independent Wnt Signaling.
Authors: Kling Et al.
Front Immunol 2018;9:483
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Mtf2-PRC2 control of canonical Wnt signaling is required for definitive erythropoiesis.
Authors: Rothberg
Cell Discov 2018;4:21
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Effect of inhibition of CBP-coactivated β-catenin-mediated Wnt signalling in uremic rats with vascular calcifications.
Authors: Gravesen
PLoS One 2018;13(8):e0201936
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Titanium particle-induced osteogenic inhibition and bone destruction are mediated by the GSK-3β/β-catenin signal pathway.
Authors: Gu Et al.
Cell Death Dis 2017;8:e2878
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β-Catenin Directs Nuclear Factor-κB p65 Output via CREB-Binding Protein/p300 in Human Airway Smooth Muscle.
Authors: Koopmans Et al.
Front Immunol 2017;8:1086
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ICG-001 affects DRP1 activity and ER stress correlative with its anti-proliferative effect.
Authors: Zinecker Et al.
Oncotarget 2017;8:106764
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Sam68 Allows Selective Targeting of Human Cancer Stem Cells.
Authors: Benoit Et al.
Cell Chem Biol 2017;24:833
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WNT ligands contribute to the immune response during septic shock and amplify endotoxemia-driven inflammation in mice.
Authors: Heinrich Et al.
Blood Adv 2017;1:1274-1286
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Integrin signalling regulates the expansion of neuroepithelial progenitors and neurogenesis via Wnt7a and Decorin.
Authors: Long Et al.
J Clin Invest 2016;7:10354
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Selective targeting of CREB-binding protein/β-catenin inhibits growth of and extracellular matrix remodelling by airway smooth muscle.
Authors: Koopmans Et al.
Br J Pharmacol 2016;173:3327
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WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited.
Authors: Boulter Et al.
PLoS One 2015;125:1269
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Non-Canonical Wnt Predominates in Activated Rat Hepatic Stellate Cells, Influencing HSC Survival and Paracrine Stimulation of Kupffer Cells.
Authors: Corbett Et al.
J Immunol 2015;10:e0142794
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A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway.
Authors: Nishiya Et al.
Chem Biol 2014;21:530
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