ICG-001

目录号: HY-14428 纯度: 99.86%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

ICG-001 是 β-catenin/TCF 介导的转录抑制剂。 ICG-001 特异性结合 CREB 蛋白起作用，IC₅₀ 为3 μM。ICG-001 选择性地阻断 β-catenin/CBP 相互作用而不干扰 β-catenin/p300 相互作用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

ICG-001 Chemical Structure

CAS No. : 780757-88-2

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1112	In-stock
5 mg	￥921	In-stock
10 mg	￥1200	In-stock
50 mg	￥4500	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 47 篇科研文献

IHC

: ICG-001 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jul 18;9(8):793. [Abstract]; BMDMs are cultured with the conditional medium (CM) that is collected from cultured Hepa1-6 cells for 24 h. Meanwhile BMDMs are treated with or without ICG001. The M2-related markers and downstream genes of Wnt signaling are detected by western blotting.

: ICG-001 purchased from MCE. Usage Cited in: Int J Mol Sci. 2018 Jul 6;19(7). pii: E1981. [Abstract]; Cells exposed to ICG-001 for 24 h under different concentrations of (0, 6, 8 μM) are analyzed by Western blot for full-length PARP and cleaved PARP, with β-actin being a loading control.

: ICG-001 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2017 Sep 11;36(1):125. [Abstract]; ICG-001 mediates the association of β-catenin with CBP, P300, E-cadherin and N-cadherin. a and b Western blotting analysis of Wnt related proteins from total proteins and extracted nuclear and cytoplasmic proteins.

: ICG-001 purchased from MCE. Usage Cited in: Oncotarget. 2017 Dec 1;8(70):115089-115101. [Abstract]; ICG001 normalizes the down expression of E-cadherin and reduces the over-expression of N-cadherin and snail in residual tumor tissue after insufficient microwave ablation (MWA).

: ICG-001 purchased from MCE. Usage Cited in: Oncotarget. 2017 Dec 1;8(70):115089-115101. [Abstract]; ICG001 depresses the heat-induced over-expression of EMT markers (N-cadherin, Snail), and partially recovers the expression of E-cadherin in heat-treated SUM-1315 and ZR-75-1 cells.

: ICG-001 purchased from MCE. Usage Cited in: Cancer Sci. 2016 Dec;107(12):1776-1784. [Abstract]; The amount of ABCC3 protein is increased by ICG-001 treatment in HT-29 cells.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC₅₀ of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.

IC₅₀ & Target

IC50: 3 μM (CBP)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	GI₅₀	6.1 μM Compound: ICG001	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 24950489]
HCT-116	IC₅₀	38 μM Compound: ICG-001	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
HCT-116	IC₅₀	38 μM Compound: ICG-001	Antiproliferative activity against beta-catenin signalling overexpressing human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against beta-catenin signalling overexpressing human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay	[PMID: 34270257]
HepG2	GI₅₀	12.7 μM Compound: ICG001	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 24950489]
HT-29	IC₅₀	10.8 μM Compound: ICG-001	Cytotoxicity against human HT-29 cells assessed as cell viability at 1.563 to 50 uM measured after 72 hrs by plate reader method Cytotoxicity against human HT-29 cells assessed as cell viability at 1.563 to 50 uM measured after 72 hrs by plate reader method	[PMID: 34062253]
HT-29	GI₅₀	17.2 μM Compound: ICG001	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 24950489]
HT-29	IC₅₀	18.7 μM Compound: ICG001	Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control	[PMID: 24950489]
LoVo	GI₅₀	15.6 μM Compound: ICG001	Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay	[PMID: 24950489]
MCF-10A	IC₅₀	21 μM Compound: ICG-001	Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
MCF-10A	IC₅₀	21 μM Compound: ICG-001	Cytotoxicity against human MCF-10A cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay Cytotoxicity against human MCF-10A cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay	[PMID: 34270257]
MDA-MB-231	IC₅₀	7.2 μM Compound: ICG-001	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
MDA-MB-231	IC₅₀	7.2 μM Compound: ICG-001	Antiproliferative activity against beta-catenin signalling overexpressing human MDA-MB-231 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against beta-catenin signalling overexpressing human MDA-MB-231 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay	[PMID: 34270257]
MDA-MB-468	IC₅₀	31 μM Compound: ICG-001	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
MDA-MB-468	IC₅₀	31 μM Compound: ICG-001	Antiproliferative activity against beta-catenin signalling overexpressing human MDA-MB-468 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against beta-catenin signalling overexpressing human MDA-MB-468 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay	[PMID: 34270257]
SW480	IC₅₀	1.3 μM Compound: ICG-001	Inhibition of CBP binding to beta-casein in human SW480 cells by immunoblot analysis Inhibition of CBP binding to beta-casein in human SW480 cells by immunoblot analysis	[PMID: 23232060]
SW480	IC₅₀	6.1 μM Compound: ICG-001	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 34382808]
SW480	IC₅₀	6.1 μM Compound: ICG-001	Antiproliferative activity against beta-catenin signalling overexpressing human SW480 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against beta-catenin signalling overexpressing human SW480 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay	[PMID: 34270257]

体外研究
(In Vitro)

ICG-001 (5 μM) 在 MCF7 细胞中抑制瘦素诱导的 EMT、侵袭和肿瘤球形成^[1]。ICG-001 可以在表型上挽救早老素 1 突变细胞中正常神经生长因子 (NGF) 诱导的神经元分化和神经元向外生长，强调了 TCF/β-catenin 信号通路对神经突向外生长和神经元分化的重要性^[2]。ICG-001 (25 μM) 处理可降低 SW480 细胞中生存素和细胞周期蛋白 D1 RNA 和蛋白质的稳态水平，这两者均可被 β-连环蛋白上调。ICG-001 在转化细胞而非正常结肠细胞中选择性诱导细胞凋亡，并减少结肠癌细胞的体外生长^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

ICG-001 (每天 5 mg/kg) 显著抑制小鼠的 β-连环蛋白信号传导，同时保护上皮细胞^[2]。施用 ICG-001 的水溶性类似物 9 周后，结肠和小肠息肉的形成减少了 42%，与非甾体类抗炎药 MK-231 一样有效，后者在该模型中一直显示出疗效。ICG-001 (150 mg/kg，静脉注射) 在 SW620 裸鼠肿瘤消退异种移植模型中显示，在 19 天的处理过程中肿瘤体积显著减少，没有死亡或体重减轻^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

548.63

Formula

C₃₃H₃₂N₄O₄

CAS 号

780757-88-2

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (91.14 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.56 mM); 悬浊液; 超声加热助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.56 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 15% Cremophor EL 85% Saline
Solubility: 1.67 mg/mL (3.04 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 17% Solutol HS-15 in Saline
Solubility: 1.67 mg/mL (3.04 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.86%

选择批次：

Data Sheet (658 KB) SDS (393 KB)

COA (201 KB) LCMS (86 KB) 元素分析报告 (217 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Yan D, et al, Leptin-induced epithelial-mesenchymal transition in breast cancer cells requires β-catenin activation via Akt/GSK3- and MTA1/Wnt1 protein-dependent pathways. J Biol Chem, 2012, 287(11), 8598-8612. [Content Brief]

[2]. Henderson WR Jr, et al, Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc Natl Acad Sci USA, 2010, 107(32), 14309-14314. [Content Brief]

[3]. Emami KH, et al. A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]. Proc Natl Acad Sci USA, 2004, 101(34), 12682-12687. [Content Brief]

[4]. Liu Y, et al. ICG-001 suppresses growth of gastric cancer cells and reduces chemoresistance of cancer stem cell-like population. J Exp Clin Cancer Res. 2017 Sep 11;36(1):125. [Content Brief]

Cell Assay ^[2]	To evaluate effects of ICG-001 on α-SMA and collagen type 1 expression, RLE-6TN cells are treated with TGF-β1 (0.25 ng/mL) in the presence or absence of ICG-001 (5.0 μM). After 24 h, cells are harvested and mRNA isolated for analysis by qPCR. RNA is reverse-transcribed using SuperScript reverse transcriptase. Quantitative PCR is performed with SYBR-Green PCR using Real-Time PCR System HT7900. The amplification protocol is set as follows: 95°C denaturation for 10 min followed by 40 cycles of 15-s denaturation at 95°C, 1 min of annealing/extension, and data collection at 60°C. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Seven-week-old male C57BL/6J-Apc^Min/+and WT C57BL/6J mice are treated orally for 9 weeks with ICG-001a (300 mg/kg per day) or vehicle (1% carboxymethylcellulose), once daily, six times per week. MK-231 is administered in drinking water (160 ppm, dissolved in 8 mM Na₂PO₄ buffer, pH 7.6). At 16 weeks, the polyp number is counted manually by using a dissecting microscope. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Yan D, et al, Leptin-induced epithelial-mesenchymal transition in breast cancer cells requires β-catenin activation via Akt/GSK3- and MTA1/Wnt1 protein-dependent pathways. J Biol Chem, 2012, 287(11), 8598-8612. [Content Brief] [2]. Henderson WR Jr, et al, Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc Natl Acad Sci USA, 2010, 107(32), 14309-14314. [Content Brief] [3]. Emami KH, et al. A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]. Proc Natl Acad Sci USA, 2004, 101(34), 12682-12687. [Content Brief] [4]. Liu Y, et al. ICG-001 suppresses growth of gastric cancer cells and reduces chemoresistance of cancer stem cell-like population. J Exp Clin Cancer Res. 2017 Sep 11;36(1):125. [Content Brief]

ICG-001 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8227 mL	9.1136 mL	18.2272 mL	45.5681 mL
	5 mM	0.3645 mL	1.8227 mL	3.6454 mL	9.1136 mL
	10 mM	0.1823 mL	0.9114 mL	1.8227 mL	4.5568 mL
	15 mM	0.1215 mL	0.6076 mL	1.2151 mL	3.0379 mL
	20 mM	0.0911 mL	0.4557 mL	0.9114 mL	2.2784 mL
	25 mM	0.0729 mL	0.3645 mL	0.7291 mL	1.8227 mL
	30 mM	0.0608 mL	0.3038 mL	0.6076 mL	1.5189 mL
	40 mM	0.0456 mL	0.2278 mL	0.4557 mL	1.1392 mL
	50 mM	0.0365 mL	0.1823 mL	0.3645 mL	0.9114 mL
	60 mM	0.0304 mL	0.1519 mL	0.3038 mL	0.7595 mL
	80 mM	0.0228 mL	0.1139 mL	0.2278 mL	0.5696 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ICG-001780757-88-2ICG001ICG 001β-cateninApoptosisBeta cateninInhibitorinhibitorinhibit

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ICG-001

Customer Review

MCE 顾客使用本产品发表的 47 篇科研文献

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•同靶点产品:

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生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

ICG-001 相关分类

完整储备液配制表

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ICG-001

Customer Review

ICG-001 相关抗体

MCE 顾客使用本产品发表的 47 篇科研文献

ICG-001 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

ICG-001 相关抗体:

摩尔计算器

稀释计算器

ICG-001 相关分类

完整储备液配制表

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