SM 16

Pricing Availability   Qty
Cat.No. 6245 - SM 16 | C25H26N4O3 | CAS No. 614749-78-9
Description: Potent TGF-βRI inhibitor; orally bioavailable
Chemical Name: 4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (5)
Pathways

Biological Activity

Potent TGF-β receptor type 1 (TGF-βRI) inhibitor (IC50 = 64 nM in luciferase assay). Selective for TGF-βRI over other ALK family members. Decreases Smad phosphorylation and inhibits tumor growth in a mouse xenograft model. Attenuates increased TGF-β signaling in retinal vessels of diabetic rats. Also prevents intimal thickening and vascular remodeling in rat carotid balloon injury model. Orally bioavailable.

Technical Data

M. Wt 430.5
Formula C25H26N4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 614749-78-9
PubChem ID 10387982
InChI Key JUHTXZGCTPDXRU-UHFFFAOYSA-N
Smiles CC1=NC(C2=C(C3=CC=C4OCOC4=C3)NC(C56CCC(CC6)(C(N)=O)CC5)=N2)=CC=C1

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.05 100

Preparing Stock Solutions

The following data is based on the product molecular weight 430.5. 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 2.32 mL 11.61 mL 23.23 mL
5 mM 0.46 mL 2.32 mL 4.65 mL
10 mM 0.23 mL 1.16 mL 2.32 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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References

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

Suzuki et al (2007) A novel small-molecule inhibitor of transforming growth factor β type I receptor kinase (SM16) inhibits murine mesothelioma tumor growth in vivo and prevents tumor recurrence after surgical resection. Cancer Res. 67 2351 PMID: 17332368

Fu et al (2008) SM16, an orally active TGF-β type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model. Arterioscler.Thromb.Vasc.Biol. 28 665 PMID: 18202322

Dagher et al (2017) The increased transforming growth factor-β signaling induced by diabetes protects retinal vessels. Am.J.Pathol. 187 627 PMID: 28162229


If you know of a relevant reference for SM 16, please let us know.

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Keywords: SM 16, SM 16 supplier, SM16, TGF-beta, transforming, growth, factor, beta, inhibitors, inhibits, ALK5, ALK4, orally, bioavailable, Receptors, 6245, Tocris Bioscience

Citations for SM 16

Citations are publications that use Tocris products.

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Reviews for SM 16

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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* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

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Stem Cells

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

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 SM 16

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.