1. Stem Cell/Wnt
    TGF-beta/Smad
  2. TGF-beta/Smad
  3. (E)-SIS3

(E)-SIS3 

Cat. No.: HY-13013 Purity: >98.0%
Handling Instructions

(E)-SIS3 is a specific, cell-permeable, and selective Smad3 inhibitor, which inhibits Smad3 phosphorylation with an IC50 of 3 µM. (E)-SIS3 also inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.

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

(E)-SIS3 Chemical Structure

(E)-SIS3 Chemical Structure

CAS No. : 521984-48-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 151 In-stock
Estimated Time of Arrival: December 31
2 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 140 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    (E)-SIS3 purchased from MCE. 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.

    (E)-SIS3 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.

    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.

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

    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.

    (E)-SIS3 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov;103:173-181.

    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.

    (E)-SIS3 purchased from MCE. Usage Cited in: Immunol Lett. 2018 Dec 10. pii: S0165-2478(18)30420-6.

    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.

    (E)-SIS3 purchased from MCE. Usage Cited in: Int J Mol Med. 2019 Feb;43(2):993-1002. 

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

    (E)-SIS3 purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Aug;20(2):1605-1612.

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

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    Description

    (E)-SIS3 is a specific, cell-permeable, and selective Smad3 inhibitor, which inhibits Smad3 phosphorylation with an IC50 of 3 µM. (E)-SIS3 also inhibits the myofibroblast differentiation of fibroblasts by TGF-β1[1][2].

    In Vitro

    (E)-SIS3 completely diminishes the constitutive phosphorylation of Smad3 as well as the up-regulates type I collagen expression in scleroderma fibroblasts. (E)-SIS3 is a useful tool to evaluate the TGF-β-regulated cellular mechanisms via selective inhibition of Smad3[2].

    Molecular Weight

    489.99

    Formula

    C₂₈H₂₈ClN₃O₃

    CAS No.

    521984-48-5

    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.[E]

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (61.23 mM)

    *"≥" means soluble, but saturation unknown.

    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: ≥ 2.5 mg/mL (5.10 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    (E)-SIS3
    Cat. No.:
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