SIS3

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Cat.No. 5291 - SIS3 | C28H27N3O3.HCl | CAS No. 521984-48-5
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: ≥98% (HPLC)
Datasheet
Citations (1)
Literature
Pathways

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.

Compound Libraries

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

Technical Data

M. Wt 489.99
Formula C28H27N3O3.HCl
Storage Store at -20°C
Purity ≥98% (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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 489.99. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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1 Citation for SIS3

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


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Pathways for SIS3

TGF-β

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.