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
Biological ActivityICG 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
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.
Citations for ICG 001
The citations listed below are publications that use Tocris products. Selected citations for ICG 001 include:
12 Citations: Showing 1 - 10
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
Mtf2-PRC2 control of canonical Wnt signaling is required for definitive erythropoiesis.
Cell Discov 2018;4:21
Effect of inhibition of CBP-coactivated β-catenin-mediated Wnt signalling in uremic rats with vascular calcifications.
PLoS One 2018;13(8):e0201936
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
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
ICG-001 affects DRP1 activity and ER stress correlative with its anti-proliferative effect.
Authors: Zinecker Et al.
Sam68 Allows Selective Targeting of Human Cancer Stem Cells.
Authors: Benoit Et al.
Cell Chem Biol 2017;24:833
Integrin signalling regulates the expansion of neuroepithelial progenitors and neurogenesis via Wnt7a and Decorin.
Authors: Long Et al.
J Clin Invest 2016;7:10354
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
WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited.
Authors: Boulter Et al.
PLoS One 2015;125:1269
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
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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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.