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Submit ReviewSD 208
Description: Potent ATP-competitive TGF-βRI inhibitor
Chemical Name: 2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine
Purity: ≥98% (HPLC)
Biological Activity for SD 208
SD 208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50 = 49 nM). Displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively. Exhibits anti-inflammatory and antitumor activity. Also promotes an antiglioma immune response. Ameliorates germinal matrix hemorrhage-induced neurological deficits in neonatal rats.
Compound Libraries for SD 208
SD 208 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for SD 208
| M. Wt | 352.75 |
| Formula | C17H10ClFN6 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 627536-09-8 |
| PubChem ID | 10316032 |
| InChI Key | BERLXWPRSBJFHO-UHFFFAOYSA-N |
| Smiles | FC(C=CC(Cl)=C3)=C3C2=NC1=NC=CN=C1C(NC4=CC=NC=C4)=N2 |
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 SD 208
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.05 | 20 with gentle warming |
Preparing Stock Solutions for SD 208
The following data is based on the product molecular weight 352.75. 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 |
|---|---|---|---|
| 0.2 mM | 14.17 mL | 70.87 mL | 141.74 mL |
| 1 mM | 2.83 mL | 14.17 mL | 28.35 mL |
| 2 mM | 1.42 mL | 7.09 mL | 14.17 mL |
| 10 mM | 0.28 mL | 1.42 mL | 2.83 mL |
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Product Datasheets for SD 208
References for SD 208
References are publications that support the biological activity of the product.
Uhl et al (2004) SD-208, a novel transforming growth factor β feceptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogeneicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 64 7954 PMID: 15520202
Kapoun et al (2006) Transforming growth factor-β receptor type I receptor (TGFβRI) kinase activity but not p38 activation is required for TGFβRI-induced myofibroblast differentiation and profibrotic gene expression. Mol.Pharmacol. 70 518 PMID: 16707625
Leung et al (2006) Effect of transforming growth factor-β receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling. J.Pharmacol.Exp.Ther. 319 586 PMID: 16888081
Manaenko et al (2014) Inhibition of transforming growth factor-β attenuates brain injury and neurological deficits in a rat model of germinal matrix hemorrhage. Stroke 45 828 PMID: 24425124
If you know of a relevant reference for SD 208, please let us know.
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Keywords: SD 208, SD 208 supplier, Potent, ATP-competitive, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1inhibitors, inhibits, Transforming, Growth, Factors, Beta, Receptors, TGF-beta, Serine/Threonine, Kinases, RSTKs, SD208, 3269, Tocris Bioscience
10 Citations for SD 208
Citations are publications that use Tocris products. Selected citations for SD 208 include:
Clements et al (2017) The Wound Microenvironment Reprograms Schwann Cells to Invasive Mesenchymal-like Cells to Drive Peripheral Nerve Regeneration. Neuron 96 98 PMID: 28957681
Armitage et al (2011) Hepcidin regulation by innate immune and infectious stimuli. Blood 118 4129 PMID: 21873546
Li and Gotlieb (2011) Transforming growth factor-β regulates the growth of valve interstitial cells in vitro. Am J Pathol 179 1746 PMID: 21851806
Wang et al (2012) Protons sensitize epithelial cells to mesenchymal transition. PLoS One 7 e41249 PMID: 22844446
Mukherjee et al (2012) Transforming growth factor-β evokes Ca2+ waves and enhances gene expression in human pulmonary fibroblasts. Am J Respir Cell Mol Biol 46 757 PMID: 22268139
Fujii et al (2018) An IL-15 superagonist/IL-15Rα fusion complex protects and rescues NK cell-cytotoxic function from TGF-β1-mediated immunosuppression. Cancer Immunol Immunother 67 675 PMID: 29392336
Pavlides et al (2016) TGF-β activates APC through Cdh1 binding for Cks1 and Skp2 proteasomal destruction stabilizing p27kip1 for normal endometrial growth. Cell Cycle 15 931 PMID: 26963853
Seliger et al (2016) MetF. inhibits proliferation and migration of glioblastoma cells independently of TGF-β2. Cell Cycle 15 1755 PMID: 27163626
Nistala et al (2010) Differential effects of alendr. and los. therapy on osteopenia and aortic aneurysm in mice with severe Marfan syndrome. PLoS One 19 4790 PMID: 20871099
Geyh et al (2018) Transforming growth factor β1-mediated functional inhibition of mesenchymal stromal cells in myelodysplastic syndromes and acute myeloid leukemia. Haematologica 103 1462 PMID: 29773599
Do you know of a great paper that uses SD 208 from Tocris? Please let us know.
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Pathways for SD 208
