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ICG 001

Catalog #: 4505
16 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4505/10
4505/50
ICG 001 | CAS No. 780757-88-2 | beta-Catenin Inhibitors
1 Image
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%

Product Details
Citations (16)
Supplemental Products
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
548.63
Formula:
C33H32N4O4
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
780757-88-2

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

  1. Icariin attenuates titanium-particle inhibition of bone formation by activating the Wnt/?-catenin signaling pathway in vivo and in vitro
    J Wang, Y Tao, Z Ping, W Zhang, X Hu, Y Wang, L Wang, J Shi, X Wu, H Yang, Y Xu, D Geng
    Sci Rep, 2016;6(0):23827.
  2. Identification of CD24 as a cancer stem cell marker in human nasopharyngeal carcinoma.
    Yang C, Wang H, Lin Y, Kumar K, Lin H, Chang C, Lu C, Huang T, Martel J, Ojcius D, Chang Y, Young J, Lai H
    PLoS ONE, 2014;9(6):e99412.
  3. Effect of inhibition of CBP-coactivated ?-catenin-mediated Wnt signalling in uremic rats with vascular calcifications
    E Gravesen, A Nordholm, M Mace, M Morevati, E Høgdall, C Nielsen, A Kjær, K Olgaard, E Lewin
    PLoS ONE, 2018;13(8):e0201936.
  4. Titanium particle-induced osteogenic inhibition and bone destruction are mediated by the GSK-3?/?-catenin signal pathway
    Y Gu, Z Wang, J Shi, L Wang, Z Hou, X Guo, Y Tao, X Wu, W Zhou, Y Liu, W Zhang, Y Xu, H Yang, F Xue, D Geng
    Cell Death Dis, 2017;8(6):e2878.
  5. WNT7A/beta-catenin signaling induces FGF1 and influences sensitivity to niclosamide in ovarian cancer.
    King M, Lindberg M, Stodden G, Okuda H, Ebers S, Johnson A, Montag A, Lengyel E, MacLean Ii J, Hayashi K
    Oncogene, 2015;34(26):3452-62.
  6. Targeting wnt signaling in colon cancer stem cells.
    De Sousa et al.
    Clin.Cancer Res., 2011;17:647
  7. A small molecule inhibitor of β-catenin/CREB-binding protein transcription.
    Emami et al.
    Proc.Natl.Acad.Sci.USA, 2004;101:12682
  8. 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

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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

  1. 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
  2. Network-Based Integration of Multi-Omics Data Identifies the Determinants of miR-491-5p Effects.
    Authors: Laurent Et al.
    Cancers (Basel)  2021;13
  3. 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
  4. 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
  5. Mtf2-PRC2 control of canonical Wnt signaling is required for definitive erythropoiesis.
    Authors: Rothberg
    Cell Discov  2018;4:21
  6. 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
  7. 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
  8. 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
  9. ICG-001 affects DRP1 activity and ER stress correlative with its anti-proliferative effect.
    Authors: Zinecker Et al.
    Oncotarget  2017;8:106764
  10. Sam68 Allows Selective Targeting of Human Cancer Stem Cells.
    Authors: Benoit Et al.
    Cell Chem Biol  2017;24:833

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