ICG-001 is a small-molecule antagonist of b-catenin/TCF-mediated transcription (IC50 = 3 uM) and specifically downregulates the expression of a subset of b-catenin/TCF-responsive genes. ICG-001 binds specifically to cyclic AMP response element-binding protein (CBP), therby disrupting interaction of CBP with b-catenin. [1] ICG-001 selectively induces apoptosis in transformed, but not normal colon cells, and reduces in vitro growth of colon carcinoma cells.
ICG-001 has also been shown to attenuate bleomycin-induced lung fibrosis in mice by selective inhibition of Wnt/b-catenin-dependent transcription. [2]
ICG-001 is believed to correct defects in neuronal stem cell differentiation by inhibition of this pathway [3] and associated polytopic protein Presenilin-1 (PS-1), which suggests potential therapies in Alzheimer's disease.
The wnt/b-catenin signalling pathway has been implicated in regulation of cancer stem cells and ICG-001 has been studied in this regard. [4]
Technical information:
| Chemical Formula: | C33H32N4O4 | |
| CAS #: | 847591-62-2;780757-88-2 | |
| Molecular Weight: | 548.63 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | (6S,9aS)-6-(4-hydroxybenzyl)-N-benzyl-8-(naphthalen-1-ylmethyl)-4,7-dioxo-hexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide | |
| Solubility: | Up to 100mM in DMSO | |
| Synonyms: | ICG-001, ICG001 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Emami et al., A small molecule inhibitor of beta-catenin/CREB-binding protein transcription. Proc. Natl. Acad. Sci. 2004, 101(34), 12682-12687. Pubmed ID: 15314234 |
| 2. | Henderson et al., Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc. Natl. Acad. Sci. 2010, 107(32), 14309-14314. Pubmed ID: 20660310 |
| 3. | Teo et al., Specific inhibition of CBP/beta-catenin interaction rescues defects in neuronal differentiation caused by a presenilin-1 mutation. Proc. Natl. Acad. Sci. 2005, 102(34), 12171-12176. Pubmed ID: 16093313 |
| 4. | Takahashi-Yanaga et al., Targeting Wnt signaling: can we safely eradicate cancer stem cells? Clin. Cancer Res. 2010, 16, 3153-3162. Pubmed ID: 20660310 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
