ICG 001

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Cat.No. 4505 - ICG 001 | C33H32N4O4 | CAS No. 780757-88-2
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)
Datasheet
Citations (12)
Reviews
Literature (1)
Pathways (1)

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.86 100
ethanol 27.43 50

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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


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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

12 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

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

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

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

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

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

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

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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

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

Wnt

Wnt Signaling Pathway

The Wnt pathway is involved in cellular differentiation and proliferation in adult tissues and also during embryogenesis. Disturbances within the pathway may lead to the formation of tumors and promote metastasis.