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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)
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 |
| InChI Key | CDKIEBFIMCSCBB-CALJPSDSSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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.
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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
Ji Young et al (2020) Proline-rich tyrosine kinase 2 mediates transforming growth factor-beta-induced hepatic stellate cell activation and liver fibrosis. Sci Rep 10 21018 PMID: 33273492
Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217 PMID: 27320041
Lin et al (2017) Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop. Oncotarget 8 110426 PMID: 29299159
Do you know of a great paper that uses SIS3 from Tocris? Please let us know.
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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
- Differentiation
- Reprogramming
- Organoid Generation
- GMP and Ancillary Material Grade Products
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
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
