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ICG 001Cat. No. 4505 |
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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 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.Licensing Information
Not for sale in the USA.Certificate of Analysis / Safety Data Sheet
References
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-response element-binding protein (CREB)-binding protein (CBP). J.Biol.Chem. 287 7026. PMID: 22241478.
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