SIS3
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
Purity: ≥97%
Biological Activity
SIS3 is a 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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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 -
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 -
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
Product Datasheets
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Citations for SIS3
The citations listed below are publications that use Tocris products. Selected citations for SIS3 include:
8 Citations: Showing 1 - 8
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Species-specific sensitivity to TGFβ signaling and changes to the Mmp13 promoter underlie avian jaw development and evolution.
Authors: Tiange Et al.
Elife 2022;11
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Down-Regulation of a Profibrotic Transforming Growth Factor-β1/Cellular Communication Network Factor 2/Matrix Metalloprotease 9 Axis by Triamcinolone Improves Idiopathic Subglottic Stenosis.
Authors: J Humberto Et al.
Am J Pathol 2021;191:1412-1430
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Fludarabine modulates expression of type VII collagen during haematopoietic stem cell transplantation for recessive dystrophic epidermolysis bullosa.
Authors: W Et al.
Br J Dermatol 2021;185:380-390
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Proline-rich tyrosine kinase 2 mediates transforming growth factor-beta-induced hepatic stellate cell activation and liver fibrosis.
Authors: Ji Young Et al.
Sci Rep 2020;10:21018
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Cub domain-containing protein 1 negatively regulates TGF-β signaling and myofibroblast differentiation.
Authors: Noskovičová Et al.
Am J Physiol Lung Cell Mol Physiol 2018;314:L695
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Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop.
Authors: Lin Et al.
Oncotarget 2017;8:110426
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Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell: Stem Cell 2016;19:217
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Lipopolysaccharide induces a fibrotic-like phenotype in endothelial cells.
Authors: Echeverría Et al.
J Cell Mol Med 2013;17:800
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