Cat. No. 5291

SIS3 C28H27N3O3.HCl [521984-48-5]

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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

Soluble to 100 mM in DMSO
>98 %
Store at -20°C

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.

Certificate of Analysis / Safety Data Sheet

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Boudreau et al (2014) Wild-type and mutant p53 differentially regulate NADPH oxidase 4 in TGF-β-mediated migration of human lung and breast epithelial cells. Br.J.Cancer 110 2569. PMID: 24714748.

Di Bernardini et al (2014) Endothelial lineage differentiation from induced pluripotent stem cells is regulated by microRNA-21 and transforming growth factor β2 (TGF-β2) pathways. J.Biol.Chem. 289 3383. PMID: 24356956.

Jinnin et al (2006) Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-β1-induced extracellular matrix expression. Mol.Pharmacol. 69 597. PMID: 16288083.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SIS3 include:

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217. PMID: 27320041.

Do you know of a great paper that uses SIS3 from Tocris? If so please let us know.

View Related Products by Product Action

Keywords: SIS3, supplier, selective, smad3, inhibitors, inhibits, TGF-beta1, TGF-B1, TGF-β1, receptors, TGF-beta2, TGF-B2, TGF-β2, TGF-betaR1, TGF-BR1, TGF-βR1, phosphorylation, stem, cells, differentiation, ipscs, induced, pluripotent, Tocris Bioscience, TGF-β Receptor products

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