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ICG-001

Chemical Structure : ICG-001

CAS No.: 780757-88-2

ICG-001 (ICG001)

Catalog No.: PC-20622Not For Human Use, Lab Use Only.

ICG-001 (ICG001) is a specific small molecule inhibitor of TCF/beta-catenin, antagonizes β-catenin/TCF-mediated transcription with IC50 of 3 uM.

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Biological Activity

ICG-001 (ICG001) is a specific small molecule inhibitor of TCF/beta-catenin, antagonizes β-catenin/TCF-mediated transcription with IC50 of 3 uM.
ICG-001 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin.
ICG-001 also does not inhibit other CBP-dependent reporters, including AP-1 and CRE (IC50>100 uM).
ICG-001 induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells.
ICG-001 inhibits the expression of the TCF/β-catenin-mediated genes survivin and cyclin D1, ICG-001 down-regulates survivin and increases caspase activity in colon carcinoma cell lines.
ICG-001 (150 mg/kg, i.v.) is efficacious in both the Min mouse and nude mouse SW620 xenograft models of cancer.

Physicochemical Properties

M.Wt 548.63
Formula C33H32N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(6S,9aS)-N-benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

References

1. Emami KH, et al. Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7.

2. Ma H, et al. Oncogene. 2005 May 19;24(22):3619-31.

3. Teo JL, et al. Proc Natl Acad Sci U S A. 2005 Aug 23;102(34):12171-6.

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