Chemical Name: 2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine
Biological ActivityPotent, 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Uhl et al.
Cancer Res., 2004;64:7954
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.
Kapoun et al.
Effect of transforming growth factor-β receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling.
Leung et al.
Inhibition of transforming growth factor-β attenuates brain injury and neurological deficits in a rat model of germinal matrix hemorrhage.
Manaenko et al.
Citations for SD 208
The citations listed below are publications that use Tocris products. Selected citations for SD 208 include:
10 Citations: Showing 1 - 10
An IL-15 superagonist/IL-15Rα fusion complex protects and rescues NK cell-cytotoxic function from TGF-β1-mediated immunosuppression.
Authors: Fujii Et al.
Cancer Immunol Immunother 2018;67:675
Transforming growth factor β1-mediated functional inhibition of mesenchymal stromal cells in myelodysplastic syndromes and acute myeloid leukemia.
Authors: Geyh Et al.
The Wound Microenvironment Reprograms Schwann Cells to Invasive Mesenchymal-like Cells to Drive Peripheral Nerve Regeneration.
Authors: Clements Et al.
TGF-β activates APC through Cdh1 binding for Cks1 and Skp2 proteasomal destruction stabilizing p27kip1 for normal endometrial growth.
Authors: Pavlides Et al.
Cell Cycle 2016;15:931
MetF. inhibits proliferation and migration of glioblastoma cells independently of TGF-β2.
Authors: Seliger Et al.
Cell Cycle 2016;15:1755
Protons sensitize epithelial cells to mesenchymal transition.
Authors: Wang Et al.
PLoS One 2012;7:e41249
Transforming growth factor-β evokes Ca2+ waves and enhances gene expression in human pulmonary fibroblasts.
Authors: Mukherjee Et al.
Am J Respir Cell Mol Biol 2012;46:757
Transforming growth factor-β regulates the growth of valve interstitial cells in vitro.
Authors: Li and Gotlieb
Am J Pathol 2011;179:1746
Hepcidin regulation by innate immune and infectious stimuli.
Authors: Armitage Et al.
Differential effects of alendr. and los. therapy on osteopenia and aortic aneurysm in mice with severe Marfan syndrome.
Authors: Nistala Et al.
PLoS One 2010;19:4790
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