1. Stem Cell/Wnt Apoptosis
  2. β-catenin Apoptosis
  3. ICG-001

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

ICG-001 Chemical Structure

CAS No. : 780757-88-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 96 In-stock
Solution
10 mM * 1 mL in DMSO USD 96 In-stock
Solid
5 mg USD 79 In-stock
10 mg USD 132 In-stock
50 mg USD 462 In-stock
100 mg USD 726 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 50 publication(s) in Google Scholar

Top Publications Citing Use of Products

44 Publications Citing Use of MCE ICG-001

WB
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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    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.
    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
    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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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.

    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)

    g

    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%

    References
    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-ApcMin/+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

    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.

    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
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    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.

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