Catalog Number: 5291
Chemical Name: 1,2,3,4-Tetrahydro-6,7-dimethoxy-2-[(2E)-3-(1-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-1-oxo-2-propenyl]-isoquinoline hydrochloride
Biological Activity
Selective Smad3 inhibitor; attenuates TGF-β1-dependent Smad3 phosphorylation and DNA binding. Has no effect on Smad2, p38 MAPK, ERK or PI 3-kinase signaling. Inhibits TGF-β1-induced myofibroblast differentiation of dermal fibroblasts. Also inhibits TGF-β2-induced endothelial cell differentiation in iPSCs.
Technical Data
  • M.Wt:
    489.99
  • Formula:
    C28H27N3O3.HCl
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    521984-48-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-β1-induced extracellular matrix expression.
    Jinnin et al.
    Mol.Pharmacol., 2006;69:597
  2. Endothelial lineage differentiation from induced pluripotent stem cells is regulated by microRNA-21 and transforming growth factor β2 (TGF-β2) pathways.
    Di Bernardini et al.
    J.Biol.Chem., 2014;289:3383
  3. Wild-type and mutant p53 differentially regulate NADPH oxidase 4 in TGF-β-mediated migration of human lung and breast epithelial cells.
    Boudreau et al.
    Br.J.Cancer, 2014;110:2569
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SIS3 include:

2 Citations: Showing 1 - 2
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  1. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell: Stem Cell 2016;19:217
  2. Lipopolysaccharide induces a fibrotic-like phenotype in endothelial cells.
    Authors: Echeverría Et al.
    J Cell Mol Med 2013;17:800

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