切换导航

ICG 001

现货
Catalog No.
A8217
Wnt/β-catenin信号通路的抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
5mg
¥ 660.00
现货
10mg
¥ 1,090.00
现货
25mg
¥ 2,540.00
现货
100mg
¥ 5,810.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

ICG001 is a small molecule inhibitor that targets Wnt/β-catenin pathway. It inhibits TCF/β-catenin mediated transcription by competing with β-catenin for CBP (CREB binding protein) but not p300 binding with an IC50 of 3 µM [1]. It can be used to specifically evaluate the role of CBP/beta-catenin association on WNT signaling and cell physiology.

ICG001 have been shown to selectively inhibit colon carcinoma cell lines (SW480 and HCT-116 cells) but not normal colonic epithelial cells (CCD-841Co). It is also efficacious in the Min mouse and nude mouse xenograft models of colon cancer [1]. ICG-001 is a potent inhibitor of GBM stem cells in culture. ICG001 selectively inhibits Wnt/beta-catenin/CREB binding protein (CBP) signaling to reverses pulmonary fibrosis and ameliorate experimental dermal fibrosis in experimental models [2,3]. ICG001 is currently in clinical trial for colon cancer and leukemias.

References:
[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. Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7.
[2]Henderson WR Jr1, 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.
[3]Beyer C, Reichert H, Akan H, Mallano T, Schramm A, Dees C, Palumbo-Zerr K, Lin NY, Distler A, Gelse K, Varga J, Distler O, Schett G, Distler JH. Blockade of canonical Wnt signalling ameliorates experimental dermal fibrosis. Ann Rheum Dis. 2013 Jul;72(7):1255-8.

文献引用

1. Zhou J, Toh SH, et al. "A loss-of-function genetic screening reveals synergistic targeting of AKT/mTOR and WTN/β-catenin pathways for treatment of AML with high PRL-3 phosphatase." J Hematol Oncol. 2018 Mar 7;11(1):36. PMID:29514683

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt548.63
Cas No.847591-62-2
FormulaC33H32N4O4
Solubility≥27.4315mg/mL in DMSO, ≥35.47 mg/mL in EtOH with ultrasonic, <2.14 mg/mL in H2O
Chemical Name(6S,9aS)-N-benzyl-6-[(4-hydroxyphenyl)methyl]-8-(naphthalen-1-ylmethyl)-4,7-dioxo-3,6,9,9a-tetrahydro-2H-pyrazino[1,2-a]pyrimidine-1-carboxamide
SDFDownload SDF
Canonical SMILESC1CN(C2CN(C(=O)C(N2C1=O)CC3=CC=C(C=C3)O)CC4=CC=CC5=CC=CC=C54)C(=O)NCC6=CC=CC=C6
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

大鼠心外膜细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10 μM;24 h

应用

用DMSO、ICG-001或IQ1处理大鼠EMCs,并进行免疫共沉淀(co-IP)试验。在DMSO处理的对照细胞中,所有的β连环蛋白与CBP相关联。IQ1对β连环蛋白共激活因子的使用影响很小。正如预期,ICG-001减少β连环蛋白/ CBP的相互作用,同时伴随β连环蛋白/ p300相互作用的增加。

动物实验[1]:

动物模型

雌性Sprague-Dawley大鼠

剂量

50 mg/kg/day;皮下注射

应用

通过手术对大鼠左冠状动脉进行永久闭塞,从而诱导左心室区域缺血性损伤。自手术当天开始,用ICG-001处理10天,手术后4周(最后一次ICG-001处理后20天)通过血管造影评估左心室射血分数,作为心脏收缩功能的指标。ICG-001显著提高8.4%的射血分数(从46.2±1.7%到54.6±3.4%,P < 0.05)。这些数据表明,在大鼠心肌梗死后,ICG-001显著改善心脏收缩功能。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Sasaki T, Hwang H, Nguyen C, et al. The small molecule Wnt signaling modulator ICG-001 improves contractile function in chronically infarcted rat myocardium. PloS one, 2013, 8(9): e75010.

生物活性

描述 ICG-001拮抗Wnt/β-catenin/TCF介导的转录,并特异性与启动子结合蛋白(CBP)相结合,IC50值为3 μM。
靶点 CBP          
IC50 3 μM          

质量控制

化学结构

ICG 001

相关生物数据

ICG 001
The COX-inhibitor ICG001 reduce dose-dependent the cell viability of HuH6 and HepT1 cells. Data represent mean ± SD of relative cell viability from triplicates. Experiments without inhibitor were set as 100 % viability.

相关生物数据

ICG 001

相关生物数据

ICG 001

相关生物数据

ICG 001