Catalog No.S2662

ICG-001 Chemical Structure

Molecular Weight(MW): 548.63

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.

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In DMSO USD 168 In stock
USD 120 In stock
USD 470 In stock
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6 Customer Reviews

  • Immunocytochemical analysis of SOX1 (a–d), SOX2 (e–h) and SOX3 (i–l) expression in NT2/D1 cells treated with either DMSO (a, b, e, f, i, j) or ICG-001 (c, d, g, h, k, l). Cell nuclei were stained with DAPI (b, d, f, h, j, l). Scale bar 50 μm.

    Histochem Cell Biol, 2015, 10.1007/s00418-015-1352-0. ICG-001 purchased from Selleck.

    ICG-001 variably influences Wnt transcriptional activity across pancreatic cancer lines. Nuclear extracts from AsPC-1 cells treated with vehicle or 30 umol/L ICG-001 for 6 hours were immunoprecipitated with anti-CBP or control IgG antibodies followed by Western blot analyses for β-catenin and CBP.

    Mol Cancer Ther 2014 13(10), 2303-14. ICG-001 purchased from Selleck.

  • J Biol Chem 2013 56(4), 423-33. ICG-001 purchased from Selleck.

    Marker protein of fibroblast-to-myofibroblast transition vimentin, a-SMA and collagen I overexpression in HELF cells caused by TGF-b1 for 24 hrs.

    J Cell Mol Med, 2017. ICG-001 purchased from Selleck.

  • Coimmunoprecipitation analysis of HCT-116 and SW620 cells treated with ICG-001. (A) Coimmunoprecipitation of HCT-116 CRC cells, using 75 uM ICG-001. Anti-CBP or anti-p300 antibody was used for the immunoprecipitation and beta-catenin was detected with an anti-beta-catenin antibody after SDS-PAGE. (B) Coimmunoprecipitation assay, similar to that described in (A), showing activity of 100 uM ICG-001 against CBP-beta-catenin association in SW620 CRC cells.

    J Cancer 2013 4(6), 481-90. ICG-001 purchased from Selleck.

    Mol Immunol 2013 56(4), 423-33. ICG-001 purchased from Selleck.

Purity & Quality Control

Choose Selective Wnt/beta-catenin Inhibitors

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.
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 NWO3dVNxSXCxcITvd4l{KEG|c3H5 NYW3TIw4PTEEoN88cS=> MWmyOOKhcA>? M1PNUWROW09? M2PNSoJtd2Otc9MgeIhmKHC{b4TlZ5RqfmViZX\m[YN1KG:oIH3lcIF1d26rbjDh[4FqdnO2IGDyVEApOTB44pETNVI3MS2rbnT1Z4VlKGGyb4D0c5Rq[yC|aXfuZYx{ M3LzO|I2OjVzMEK4
AsPC-1 M3n4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqxMVIxKM7:TR?= NXHBWm14Oi92L{[g[C=> MnTRbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mo\1NlUxQDJ7NkC=
MiaPaCa-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKxMVIxKM7:TR?= NX\CPVFpOi92L{[g[C=> MWnpcohq[mm2czD0bIUh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXiyOVA5Ojl4MB?=
PANC-1 NFHiSHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe1UHZFOS1{MDFOwG0> Mny1Nk81NzZiZB?= NGnRd5VqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MkfDNlUxQDJ7NkC=
L3.6pl M1TFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nyTlEuOjBizszN NHXEOIUzNzRxNjDk NH6xSohqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= Mnn4NlUxQDJ7NkC=
SH-SY5Y M1nF[GFxd3C2b4Ppd{BCe3OjeR?= MkKyNVAh|ryP NFfKfW4zPCCq NF3EdXZqdmirYnn0d{B1cGVibnX1do9xem:2ZXP0bZZmKGWoZnXjeJMhd2ZiaInwc5hq[SCjZ3HpcpN1KFC{UDCoNVA3NTF{NjmtcYVlcWG2ZXSgcoV2em:wYXygZ4VtdCCmZXH0bC=> NFy0W4ozOzlyMEW2Oi=>
HKC-8  Ml35SpVv[3Srb36gRZN{[Xl? Mm\pNVDDqML3TR?= M2jwXlI1KGh? NG\jeGdi[m:uaYPo[ZPDqM7{LXPheIVvcW8kgKPt[YRq[XSnZDDSRXMhcW6mdXP0bY9v MXyyOVAyOjF4Nh?=
MCF7 MkLQSpVv[3Srb36gRZN{[Xl? NWfK[GdtPSEQvH5CpC=> NF3IdlNqdmirYnn0d{Bt\XC2aX6tcYVlcWG2ZXSgbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZiU37hbYwtKFOudXesJIFv\CCcZXKy NXfPSWxlOjJ{N{CzOVk>
RLE-6TN  MVTGeY5kfGmxbjDBd5NigQ>? NF7Ydm4zNjVxNT:3MlUh|ryP MnvZOFghcA>? M3PPNYlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDFOtU1UVUFiaX7keYN1cW:wIHHu[EBGVVR? MlK1NlIzPDF2N{i=
HKC-8 NITNdXVHfW6ldHnvckBCe3OjeR?= MnnkOU8yOC9{MDFOwG0> M1Gyc|Q5KGh? NITFfmZjdG:la4Og{tIu[2G2ZX7pck1lemm4ZX6g[4Vv\SCneIDy[ZN{cW:w M2jmU|IyQDF4OUO3
SW480 NHnRcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG1Tm4zNTFyMDFOwG0> MorZTWM2OD13LklCtVAvPjhizszN MWCxOVc5OjF|OB?=

... Click to View More Cell Line Experimental Data

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/+
  • Formulation: Water-soluble analog of ICG-001 is used.
  • 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)
Ethanol 10 mg/mL (18.22 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+50% PEG 300+5% Tween 80+ddH2O

* 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
Storage powder
Synonyms N/A

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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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID