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Description: Selective Smad3 inhibitor; inhibits TGF-βR1 signaling
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% (HPLC)
Citations (7)
Literature (3)
Pathways (1)

Biological Activity for SIS3

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.

Compound Libraries for SIS3

SIS3 is also offered as part of the Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for SIS3

M. Wt 489.99
Formula C28H27N3O3.HCl
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 521984-48-5
PubChem ID 16079005
Smiles O=C(N4CCC(C=C(OC)C(OC)=C5)=C5C4)/C=C/C2=C(C3=CC=CC=C3)N(C)C1=NC=CC=C12.Cl

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.

Solubility Data for SIS3

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 49 100

Preparing Stock Solutions for SIS3

The following data is based on the product molecular weight 489.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.04 mL 10.2 mL 20.41 mL
5 mM 0.41 mL 2.04 mL 4.08 mL
10 mM 0.2 mL 1.02 mL 2.04 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets for SIS3

Certificate of Analysis / Product Datasheet
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References for SIS3

References are publications that support the biological activity of the product.

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

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

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

If you know of a relevant reference for SIS3, please let us know.

Keywords: SIS3, 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, Other, Transcription, Factors, TGF-beta, Receptors, Differentiation, Products, 5291, Tocris Bioscience

7 Citations for SIS3

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

J Humberto et al (2021) Down-Regulation of a Profibrotic Transforming Growth Factor-β1/Cellular Communication Network Factor 2/Matrix Metalloprotease 9 Axis by Triamcinolone Improves Idiopathic Subglottic Stenosis. Am J Pathol 191 1412-1430 PMID: 34111429

W et al (2021) Fludarabine modulates expression of type VII collagen during haematopoietic stem cell transplantation for recessive dystrophic epidermolysis bullosa. Br J Dermatol 185 380-390 PMID: 33368156

Tiange et al (2022) Species-specific sensitivity to TGFβ signaling and changes to the Mmp13 promoter underlie avian jaw development and evolution. Elife 11 PMID: 35666955

Noskovičová et al (2018) Cub domain-containing protein 1 negatively regulates TGF-β signaling and myofibroblast differentiation. Am J Physiol Lung Cell Mol Physiol 314 L695 PMID: 29351434

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

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

  • Self-renewal and Maintenance
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Stem Cells Scientific Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for SIS3

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.