2. Stem Cell/Wnt TGF-beta/Smad
  3. TGF-beta/Smad
  4. SIS3

(E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.

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

SIS3 Chemical Structure

SIS3 Chemical Structure

CAS No. : 521984-48-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 151 In-stock
Solution
10 mM * 1 mL in DMSO USD 151 In-stock
Solid
2 mg USD 66 In-stock
5 mg USD 140 In-stock
10 mg USD 215 In-stock
25 mg USD 440 In-stock
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Customer Review

Based on 82 publication(s) in Google Scholar

Other Forms of SIS3:

SIS3 Related Antibodies

Top Publications Citing Use of Products

75 Publications Citing Use of MCE SIS3

WB

    SIS3 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Aug;20(2):1605-1612.  [Abstract]

    SIS3 treatment decreases the TGFβ1-induced expression of Col I and FN.

    SIS3 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836.  [Abstract]

    NRK-49F cells are preincubated with 100 nM, 10 μM, or 50 μM Smad3 inhibitor SIS3 for 30 min followed by TGF-β1 (2 ng/mL) stimulation for 12 h. Then, the expression of Sphk2, fibronectin, and α-SMA is determined by Western blotting.

    SIS3 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.  [Abstract]

    By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

    SIS3 purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2019 Feb;43(2):993-1002.   [Abstract]

    Western analysis of FN expression in HUVECs pretreated with PD98059 and SIS3.

    SIS3 purchased from MedChemExpress. Usage Cited in: Immunol Lett. 2019 Feb;206:33-40.  [Abstract]

    Monocytes were cultured with 20 ng/mL M-CSF with or without 10 ng/mL TGF-β1 for 2 days, with SB431542 (1 or 50 μM) or SIS3 (2.5 μM) having been added 30 min beforehand. Whole-cell lysates were subjected to SDS-PAGE and immunoblotted.

    SIS3 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2018 Nov;103:173-181.  [Abstract]

    TRPM7 mRNA and protein expressions are effectively suppressed by LY2109761 and SIS3 in ASMCs compared with those in 10 ng/mL TGF-β1-stimulated cells.

    SIS3 purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Med. 2016;9(8):15892-15899.

    CNE1 cells are cultured with 3 μM SIS3 for 4 hs, and then washed by cold PBS and followed by the 10 ng/mL TGF-β treatments for 48 hs, respectively.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    (E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1[1].

    IC50 & Target

    IC50: 3 μM (Smad3 phosphorylation)[1]
    In Vitro

    (E)-SIS3 (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4[1].
    (E)-SIS3 (0.1?, 10, 50?μM; 30?min) significantly suppresses the expression of FN and α-SMA, but not that of Sphk2 provoked by TGF-β1[2].
    (E)-SIS3 (10 μM; 24 hours) significantly reduces both α-SMA and palladin expression that is enhanced by TWEAK in Primary human dermal fibroblasts[3].
    (E)-SIS3 significantly inhibits L4 development at five concentrations from as low as 2 μM to 50 μM (5 μM, 10 μM, 20 μM and 50 μM) in a dose-dependent manner[4].

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

    SIS3 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: Human dermal fibroblasts
    Concentration: 0.3, 1, 3, 10 μM
    Incubation Time: For 1 hour
    Result: Attenuated the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4.
    Molecular Weight

    489.99

    Formula

    C28H28ClN3O3
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    [H]Cl.O=C(/C=C/C1=C(N(C2=NC=CC=C21)C)C3=CC=CC=C3)N4CC5=C(CC4)C=C(C(OC)=C5)OC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (204.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0409 mL 10.2043 mL 20.4086 mL
    5 mM 0.4082 mL 2.0409 mL 4.0817 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 (sealed storage, away from moisture). 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 (5.10 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      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 (5.10 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL. 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).

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    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: 98.71%

    COA (253 KB) HNMR (273 KB) RP-HPLC (248 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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 (sealed storage, away from moisture). 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 2.0409 mL 10.2043 mL 20.4086 mL 51.0215 mL
    5 mM 0.4082 mL 2.0409 mL 4.0817 mL 10.2043 mL
    10 mM 0.2041 mL 1.0204 mL 2.0409 mL 5.1021 mL
    15 mM 0.1361 mL 0.6803 mL 1.3606 mL 3.4014 mL
    20 mM 0.1020 mL 0.5102 mL 1.0204 mL 2.5511 mL
    25 mM 0.0816 mL 0.4082 mL 0.8163 mL 2.0409 mL
    30 mM 0.0680 mL 0.3401 mL 0.6803 mL 1.7007 mL
    40 mM 0.0510 mL 0.2551 mL 0.5102 mL 1.2755 mL
    50 mM 0.0408 mL 0.2041 mL 0.4082 mL 1.0204 mL
    60 mM 0.0340 mL 0.1701 mL 0.3401 mL 0.8504 mL
    80 mM 0.0255 mL 0.1276 mL 0.2551 mL 0.6378 mL
    100 mM 0.0204 mL 0.1020 mL 0.2041 mL 0.5102 mL
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    SIS3 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:

    SIS3521984-48-5SIS 3SIS-3TGF-beta/SmadTransforming growth factor betaSmad3phosphorylationmyofibroblastdifferentiationfibroblastsTGF-β1Inhibitorinhibitorinhibit

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