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

产品信息

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.
ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC₅₀ of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC₅₀s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.
In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

CAS号	868774-16-7
分子式	C33H32N4O4
主要靶点	β-catenin
主要通路	Stem Cells/Wnt
分子量	548.6316
MDL NO	MFCD12032107
Pubchem ID	11295786.0
纯度	99.97%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件	粉末 -20°C 3年 液体 -80°C 1年
运输条件	Shipped in cold pack
别名

靶点

Target	Activity
Wnt/β-catenin/CBP	IC50=3μM

溶解度

DMSO	600 mg/mL
Water	insoluble

细胞研究

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
AsPC-1	1-20 μM	Growth Inhibition Assay	2/4/6 d	inhibits the cell growth in a dose-dependent manner	25082960
HepT1	0-100 μM	Apoptosis Assay	24 h	IC50=34 μM	23266718
HK-2	10 µM	Function Assay	3 h	reduced the expression of TGF-β1, α-SMA, and CTGF after treatment with HHE	23690997
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动物实验配方

Administration	Formulation	Solubility	Status
IP	2% DMSO+2% Tween80+40% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	50 mg/mL	suspension