For research use only.

Catalog No.S2662

109 publications

ICG-001 Chemical Structure

CAS No. 780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)

ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.

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10mM (1mL in DMSO) USD 168 In stock
USD 120 In stock
USD 470 In stock
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Selleck's ICG-001 has been cited by 109 publications

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Biological Activity

Description ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.
CBP [1]
(Cell-free assay)
3 μM
In vitro

ICG-001 has no effect on the related reporter construct, FOPFLASH, which contains mutated TCF sites. After treatment with 25μM of ICG-001 for 8 hours, SW480 cell reduces the steady-state levels of Survivin and Cyclin D1 RNA and protein, both of which can be up-regulated by β-catenin. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma 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] A recent study demonstrates that 5μM ICG-001 inhibits leptin-induced EMT, invasion and tumorsphere formation in MCF7 cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y NXTQNFg4SXCxcITvd4l{KEG|c3H5 Mmm0OVDDqM7:bR?= NWC1e3liOjUEoHi= M3HvfWROW09? NILNOJNjdG:la4RCpJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDt[YxifG:waX6gZYdicW6|dDDQdnAhMDFyNvMAl|EzPilvaX7keYNm\CCjcH;weI91cWNic3nncoFtew>? MWiyOVI2OTB{OB?=
AsPC-1 M{DSOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfsOJFMOS1{MDFOwG0> NWS4RZpVOi92L{[g[C=> NU[xfIc3cW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MYOyOVA5Ojl4MB?=
MiaPaCa-2 M3fy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfKdJV4OS1{MDFOwG0> NF:5WoczNzRxNjDk MXnpcohq[mm2czD0bIUh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUCyOVA5Ojl4MB?=
PANC-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfaPFVEOS1{MDFOwG0> NHK4OpkzNzRxNjDk NETzfnhqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NXXCS|lZOjVyOEK5OlA>
L3.6pl M3;GO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvrNU0zOCEQvF2= M1z6W|IwPC94IHS= M4LsUYlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MoK0NlUxQDJ7NkC=
SH-SY5Y NH\yeI9CeG:ydH;zbZMhSXO|YYm= NFX6Zm4yOCEQvF2= M2XDXVI1KGh? M4T5e4lvcGmkaYTzJJRp\SCwZYXyc5Bzd3SnY4TpeoUh\W[oZXP0d{Bw\iCqeYDvfIliKGGpYXnud5QhWHKSIDixNFYuOTJ4KT3t[YRq[XSnZDDu[ZVzd26jbDDj[YxtKGSnYYTo Mn36NlM6ODB3Nk[=
HKC-8  MmjISpVv[3Srb36gRZN{[Xl? NYPwcYI5OTEEoNM1US=> NUPrPJp7OjRiaB?= NVHGOIJk[WKxbHnzbIV{yqEQsj3jZZRmdmmw4pETcYVlcWG2ZXSgVmFUKGmwZIXjeIlwdg>? NV;rWYJpOjVyMUKxOlY>
HepT1 NXXQbJppSXCxcITvd4l{KEG|c3H5 M{n6WlAuOTBywrFOwG0> MnjqNlQhcA>? M4frV2lEPTB;M{VCpO69VQ>? M1n3NVI{OjZ4N{G4
HuH6 NYTxdIN1SXCxcITvd4l{KEG|c3H5 MXywMVExOMLizszN NXPkZXFjOjRiaB?= MlK2TWM2OD1|OdMg{txO NXfrdYY{OjN{Nk[3NVg>
MCF7 MV\GeY5kfGmxbjDBd5NigQ>? NYnMSpJpPSEQvH5CpC=> MYnpcohq[mm2czDs[ZB1cW5vbXXkbYF1\WRiaX7jdoVie2WmIHX4dJJme3Orb36gc4YhW26jaXysJHNtfWduIHHu[EBb\WJ{ MVqyNlI4ODN3OR?=
RLE-6TN  MXXGeY5kfGmxbjDBd5NigQ>? NGHY[HUzNjVxNT:3MlUh|ryP MY[0PEBp MYTpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRizsGtV21CKGmwZIXjeIlwdiCjbnSgSW1V M1e4ZlIzOjRzNEe4
HKC-8 M4DIemZ2dmO2aX;uJGF{e2G7 MWC1M|ExNzJyIN88US=> M1LF[FQ5KGh? NUewWnEy[myxY3vzJO6zNWOjdHXubY4u\HKrdnXuJIdmdmViZYjwdoV{e2mxbh?= NFTETWUzOThzNkmzOy=>
SW480 MnPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHF[4wzNTFyMDFOwG0> M1jKVGlEPTB;NT64xtExNjZ6IN88US=> NIf3N5oyPTd6MkGzPC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
CCNB1 / Cyclin D1 ; 

PubMed: 28893318     

ICG-001 reduced expression of CCNB1 and CyclinD1 in MGC-803. Data are the mean ± SEM of three independent experiments.

ABC / Beta-catenin / E-cadherin / N-cadherin / MMP-9 / c-MYC / Actin / Histone H3; 

PubMed: 28893318     

Western blotting analysis of Wnt related proteins from total proteins and extracted nuclear and cytoplasmic proteins.

beta-catenin / F-actin; 

PubMed: 28893318     

Confocal analysis of the expression and distribution of β-catenin in MGC-803 with or without ICG-001.


PubMed: 29986466     

Cells were exposed to ICG-001 for 24 h at the indicated concentrations and with DMSO as control, and cell lysates were probed with phosphor- and total antibodies of β-catenin signaling pathway. β-actin was used as a loading control. The representative ima䲧疝Ỵ疞㧀疜膉痘 

SOX-2 / CD44 / Survivin / EGFR / FOXM1 / EZH2 / Vimentin; 

PubMed: 25897700     

In EBV-positive C666-1 cells, (b) Western blotting analysis of SOX2, CD44, Survivin, EGFR, FOXM1, and EZH2 expression on day-7. (c) Western blotting analysis of epithelial-mesenchymal transition (EMT) markers, E-cadherin and vimentin on day-7. 

28893318 29986466 25897700
In vivo 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 Sulindac, which has consistently demonstrated efficacy in this model. No overt toxicity is detected throughout the course of treatment. In the SW620 nude mouse xenograft model of tumor regression, 150 mg/kg, i.v. of analog demonstrates a dramatic reduction in tumor volume over the 19-day course of treatment, with no mortality or weight loss. [1] ICG-001 (5 mg/kg per day) significantly inhibits beta-catenin signaling and attenuates bleomycin-induced lung fibrosis in mice, while concurrently preserving the epithelium. [4]


Kinase Assay:[1]
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DUAL-Luciferase Reporter Assay:

The Dual-Luciferase Reporter (DLR) Assay System provides an efficient means of performing dual reporter assays. In the DLRTM Assay, the activities of firefly (Photinus pyralis) and Renilla (Renilla reniformis, also known as sea pansy) luciferases are measured sequentially from a single sample. The firefly luciferase reporter is measured first by adding Luciferase Assay Reagent II (LAR II) to generate a “glow-type” luminescent signal. After quantifying the firefly luminescence, this reaction is quenched, and the Renilla luciferase reaction is initiated by simultaneously adding Stop & Glo® Reagent to the same tube. The Stop & Glo® Reagent also produces a “glow-type” signal from the Renilla luciferase, which decays slowly over the course of the measurement. In the DLRTM Assay System, both reporters yield linear assays with subattomole (<10-18) sensitivities and no endogenous activity of either reporter in the experimental host cells. Furthermore, the integrated format of the DLRTM Assay provides rapid quantitation of both reporters either in transfected cells or in cell-free transcription/translation reactions.
Cell Research:[1]
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  • Cell lines: Human colon carcinoma cell lines SW480, SW620, and HCT116, normal colonic epithelial cell line CCD-841Co
  • Concentrations: ~25 μM
  • Incubation Time: 24 hours
  • Method: 1. Prior to starting the assay, prepare the Apo-ONE Caspase-3/7 Reagent, and mix thoroughly. 2. For best results, empirical determination of the optimal cell number, apoptosis induction treatment and incubation period for the cell culture system may be necessary. 3. Use identical cell numbers and volumes for the assay and the negative control samples. 4. Do not mix Apo-ONE Caspase-3/7 Reagent and samples by manual pipetting. Mixing in this manner is unnecessary and may create bubbles that interfere with fluorescence readings or cross-contaminate the samples. Gentle mixing may be performed using a plate shaker. 5. Total incubation time for the assay depends upon the amount of caspase- 3/7 present in the sample. 6. The Apo-ONE Caspase-3/7 Reagent is formulated to mediate cellular lysis and support optimal caspase-3/7 activity. In rare instances, the reagent does not affect complete lysis of cultured cells. In such cases, lysis is enhanced by a freeze-thaw cycle. For best results, freeze at -70 °C, then thaw at room temperature. After equilibration, mix to homogeneity and incubate until measurable fluorescence is achieved
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Seven-week-old male C57BL/6J-Apc Min/+
  • Dosages: 300 mg/kg
  • Administration: Water-soluble analog of ICG-001 is treated orally for 9 weeks everyday.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (182.27 mM)
Water Insoluble
Ethanol '10 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+50% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 548.63


CAS No. 780757-88-2 (relative stereochemistry); 847591-62-2 (absolute stereochemistry)
Storage powder
in solvent
Synonyms N/A
Smiles C1CN(C2CN(C(=O)C(N2C1=O)CC3=CC=C(C=C3)O)CC4=CC=CC5=CC=CC=C54)C(=O)NCC6=CC=CC=C6

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    If the compound is stored in DMSO at -80, how long would it be stable? For cell culture, how long should I change for the fresh medium with ICG-001?

  • Answer:

    The product in DMSO solution can be stored at 4 degree for 1 week and -20 degree for 1 month. The best storage condition is solid powder, even at -80 the solution is not stable enough for long term storage. For cell culture, you need change medium every 48h.

Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID