2. Stem Cell/Wnt Apoptosis
  3. Wnt Apoptosis
  4. iCRT3

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.

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iCRT3 Chemical Structure

iCRT3 Chemical Structure

CAS No. : 901751-47-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

iCRT3 Related Antibodies

Top Publications Citing Use of Products

    iCRT3 purchased from MedChemExpress. Usage Cited in: IUBMB Life. 2023 Feb 21.  [Abstract]

    iCRT3 (10 ug/mL; 48 h) significantly lowers mRNA levels of glycolytic genes (Fig 4), as well as reduces glucose uptake (Fig i) and lactate production (Fig j) in HeLa cells.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.

    IC50 & Target

    Wnt[1], β-catenin-responsive transcription[2]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    2.4 μM
    Compound: 8, iCRT3
    Inhibition of interaction of beta-catenin (unknown origin) transfected in Wnt-activated HEK293 cells/Tcf4 assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
    Inhibition of interaction of beta-catenin (unknown origin) transfected in Wnt-activated HEK293 cells/Tcf4 assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
    		[PMID: 25985283]
    SW480 IC50
    1.1 μM
    Compound: 8, iCRT3
    Inhibition of beta-catenin/Tcf4 interaction in human SW480 cells assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
    Inhibition of beta-catenin/Tcf4 interaction in human SW480 cells assessed as decrease in transactivation of canonical Wnt signaling by TOPflash luciferase reporter assay
    		[PMID: 25985283]
    In Vitro

    iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription. iCRT3 significantly decreases TOP Flash activity and reduces the level of NTSR1. The anti-apoptotic effects of Neurotensin (NTS) and Wnt3a can be largely abrogated by iCRT3[1]. Cells maintained long term with iCRT3 show enhanced expression of classic pluripotency genes compare with the DMSO control, whereas expression of differentiation markers and T-cell factor (TCF) target genes is concomitantly reduced[2]. Treatment with iCRT3 at doses of 12.5, 25, 50, and 75 μM decreases TNF-α levels by 14.7%, 18.5%, 44.9% and 61.3%, respectively. With iCRT3 treatment, IκB levels are increased in a dose-dependent manner compare to the vehicle[3].

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

    iCRT3 Related Antibodies
    In Vivo

    The tumor growth rates are markedly retarded by iCRT3 treatment. Consistently, the tumor-suppressive role of iCRT3 is accompanied with a reduction in Ki67 index, a proliferation marker[1]. The IL-6 levels in the 10 mg/kg iCRT3 treatment group are 82.9% lower than those in the vehicle group. IL-1β levels are undetectable in the sham but reach 371 pg/mL in septic mice and are down by 30.2% and 53.2%, respectively, with 5 and 10 mg/kg iCRT3. With iCRT3 treatment at doses of 5 and 10 mg/kg, AST levels in these septic mice are 15.4% and 44.2% lower, respectively, than those in the vehicle-treated mice. After treatment with 10 mg/kg iCRT3, lung morphology is improved with much reduced microscopic deterioration, compare to the vehicle group. The number of apoptotic cells in the lung tissues of the iCRT3-treated mice is significantly reduced by 92.7% in comparison with the vehicle group[3].

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

    394.53

    Formula

    C23H26N2O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NCCC1=CC=CC=C1)CSCC2=C(C)OC(C3=CC=C(CC)C=C3)=N2
    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 : 150 mg/mL (380.20 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5347 mL 12.6733 mL 25.3466 mL
    5 mM 0.5069 mL 2.5347 mL 5.0693 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
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    Concentration
    ×
    Volume
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    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

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    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 (6.34 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.34 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.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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: 99.55%

    SDS (416 KB)

    COA (244 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells are seeded into 96-well plates to a density of 5×103 cells per well and incubated in the culture medium with iCRT3 for an additional 48 h. Cell viability and cell apoptosis assays are carried out using a Cell Counting kit-8 and a Caspase-Glo 3/7 assay kit according to the manufacturer’s instructions, respectively[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    NOD-SCID BALB/c mice are inoculated subcutaneously in the right back with 2×106 A172 cells. The growth of the primary tumors is recorded every 4 days. iCRT3 (5 mg/kg) is diluted in PBS i.p. triweekly when tumors grow to ~200 mm3. The control mice are treated with blank PBS containing 5% (v/v) DMSO. Tumor volume is evaluated with the following formula: volume=tumor length×width2/2. The mice are sacrificed 24 days after pharmaceutical treatment. The tumors are resected and embedded in paraffin, and the Ki67 staining is analyzed by immunohistochemistry[1].

    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 2.5347 mL 12.6733 mL 25.3466 mL 63.3665 mL
    5 mM 0.5069 mL 2.5347 mL 5.0693 mL 12.6733 mL
    10 mM 0.2535 mL 1.2673 mL 2.5347 mL 6.3367 mL
    15 mM 0.1690 mL 0.8449 mL 1.6898 mL 4.2244 mL
    20 mM 0.1267 mL 0.6337 mL 1.2673 mL 3.1683 mL
    25 mM 0.1014 mL 0.5069 mL 1.0139 mL 2.5347 mL
    30 mM 0.0845 mL 0.4224 mL 0.8449 mL 2.1122 mL
    40 mM 0.0634 mL 0.3168 mL 0.6337 mL 1.5842 mL
    50 mM 0.0507 mL 0.2535 mL 0.5069 mL 1.2673 mL
    60 mM 0.0422 mL 0.2112 mL 0.4224 mL 1.0561 mL
    80 mM 0.0317 mL 0.1584 mL 0.3168 mL 0.7921 mL
    100 mM 0.0253 mL 0.1267 mL 0.2535 mL 0.6337 mL
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    iCRT3 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:

    iCRT3901751-47-1iCRT 3iCRT-3WntApoptosisInhibitorinhibitorinhibit

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