ChemLeader Biomedical Co., Limited

Product Name: ICG-001(ICG 001)

CAS No.: 847591-62-2

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

Molecular Formula: C33H32N4O4

Molecular Weight: 548.63

Appearance:White or white crystallinepowder

Purity(by HPLC): >98%

Biological Activity:

ICG-001 is a selective Wnt/-cateninsignalling inhibitor with an IC50 of 3M. Inhibitor of TCF/-catenin-mediatedtranscription. Selectively inhibits -catenin/CBP interaction; displays noeffect on -catenin/p300 interaction. Exhibits growth inhibitory effects incolon carcinoma cell lines (SW480 and HCT-116 cells); also displays efficacy inMin mouse and nude mouse SW620 xenograft models.

Description: A specific inhibitor ofWnt/-catenin signaling pathway. It down-regulates beta-catenin/T cell factorsignaling by specifically binding to cyclic AMP response element-bindingprotein (CBP).  ICG-001 selectivelyinduces apoptosis in transformed cells but not in normal colon cells, reducesin vitro growth of colon carcinoma cells, and is efficacious in the Min mouseand nude mouse xenograft models of colon cancer. Specific inhibitor ofWnt/-catenin signaling pathway; inhibiting -catenin/cyclic AMP responseelement-binding (CREB) protein transcription. ICG-001 selectively inducesapoptosis in transformed cells but not in normal colon cells, reduces in vitrogrowth of colon carcinoma cells, and is efficacious in the Min mouse and nudemouse xenograft models of colon cancer.