ICG-001

Name: ICG-001
Brand: MedChemExpress
SKU: HY-14428
Rating: 5.0 (53 reviews)

Cat. No.: HY-14428 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

ICG-001 Chemical Structure

CAS No. : 780757-88-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 96	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 96	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 462	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 726	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 53 publication(s) in Google Scholar

47 Publications Citing Use of MCE ICG-001

IHC

: ICG-001 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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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Biological Activity
Protocol
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References
Customer Review

Description

IC₅₀ & Target

IC50: 3 μM (CBP)

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]

In Vitro

ICG-001 (5μM) inhibits leptin-induced EMT, invasion and tumorsphere formation in MCF7 cells^[1].?ICG-001 can phenotypically rescue normal nerve growth factor (NGF)-induced neuronal differentiation and neurite outgrowth in the presenilin-1 mutant cells, emphasizing the importance of the TCF/β-catenin signaling pathway on neurite outgrowth and neuronal differentiation^[2]. ICG-001 (25μM) treatment reduces the steady-state levels of Survivin and Cyclin D1 RNA and protein in SW480 cells, both of which can be up-regulated by β-catenin. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, and reduces in vitro growth of colon carcinoma cells^[3].

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

In Vivo

ICG-001 (5 mg/kg per day) significantly inhibits beta-catenin signaling in mice, while concurrently preserving the epithelium^[2].?Administration of a water-soluble analog of ICG-001 for 9 weeks reduces the formation of colon and small intestinal polyps by 42% as effectively as the nonsteroidal antiinflammatory agent MK-231, which has consistently demonstrated efficacy in this model. ICG-001 (150 mg/kg, i.v.) demonstrates a dramatic reduction in tumor volume over the 19-day course of treatment, with no mortality or weight loss in the SW620 nude mouse xenograft model of tumor regression^[3].

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

Molecular Weight

548.63

Formula

C₃₃H₃₂N₄O₄

CAS No.

780757-88-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=CC=CC=C1)N2CCC(N([C@@]2(CN(C3=O)CC4=C5C=CC=CC5=CC=C4)[H])[C@H]3CC6=CC=C(C=C6)O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (91.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.56 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 1.67 mg/mL (3.04 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 17% Solutol HS-15 in Saline
Solubility: 1.67 mg/mL (3.04 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (257 KB) LCMS (86 KB) Elemental Analysis Report (115 KB)

Handling Instructions (2659 KB)

References

[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.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

ICG-001 Related Classifications

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

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ICG-001 Related Antibodies

47 Publications Citing Use of MCE ICG-001

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