|(6S)-N-苄基-6-(4-羟基苄基-6-(4-萘-1-基甲基-6-(4-二氧代六氢-2H-吡嗪并[1,2-a]嘧啶-1(6H)-甲酰胺|CsnPharm

CAS No.: 868774-16-7

(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide Catalog No. CSN12696

Synonyms: N/A

ICG-001 is an inhibitor of β-catenin/cyclic AMP responsive element binding protein binding protein (CBP)-mediated transcription with IC50 of 3 µM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Wnt/β-catenin/CBP

IC50:3μM
描述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^[1]. the inhibitory IC₅₀ of ICG-001 against β-catenin/CREB mediated transcription was 3 μM^[1]. 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^[1]. 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^[1]. 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^[1]. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis^[2]. 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^[3].
细胞研究

Cell Data

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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参考文献

[1] Emami KH, Nguyen C, Ma H, Kim DH, Jeong KW, Eguchi M, Moon RT, Teo JL, Kim HY, Moon SH, Ha JR, Kahn M. A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]. Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7. doi: 10.1073/pnas.0404875101. Epub 2004 Aug 16. Erratum in: Proc Natl Acad Sci U S A. 2004 Nov 23;101(47):16707. PMID: 15314234; PMCID: PMC515116.
[2] Henderson WR Jr, Chi EY, Ye X, Nguyen C, Tien YT, Zhou B, Borok Z, Knight DA, Kahn M. Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14309-14. doi: 10.1073/pnas.1001520107. Epub 2010 Jul 21. PMID: 20660310; PMCID: PMC2922550.
[3] Sasaki T, Hwang H, Nguyen C, Kloner RA, Kahn M. The small molecule Wnt signaling modulator ICG-001 improves contractile function in chronically infarcted rat myocardium. PLoS One. 2013 Sep 12;8(9):e75010. doi: 10.1371/journal.pone.0075010. PMID: 24069374; PMCID: PMC3771968.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8227 mL
- 9.1136 mL
- 18.2272 mL
- 5 mM
- 0.3645 mL
- 1.8227 mL
- 3.6454 mL
- 10 mM
- 0.1823 mL
- 0.9114 mL
- 1.8227 mL

技术信息

CAS号

868774-16-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H32N4O4

运输

蓝冰

分子量

548.63

别名

N/A

溶解度

DMSO	600.0 mg/mL (1093.6 mM) warming
Water	insoluble

动物实验配方

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

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(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide Catalog No. CSN12696

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