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

SIS3 

Cat. No.: HY-13013 Purity: 98.02%
COA Handling Instructions

(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
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 75 publication(s) in Google Scholar

Other Forms of SIS3:

SIS3 Related Antibodies

Top Publications Citing Use of Products

68 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

    Appearance

    Solid

    Formula

    C28H28ClN3O3
    CAS No.
    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 : 125 mg/mL (255.11 mM; Need ultrasonic)

    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
    10 mM 0.2041 mL 1.0204 mL 2.0409 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 98.02%

    COA (253 KB) HNMR (271 KB) LCMS (101 KB)

    Handling Instructions (2659 KB)
    References
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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.

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    × = ×
    C1   V1   C2   V2

    Keywords:

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

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