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SD 208

Catalog #: 3269
10 Citations Datasheet / COA / SDS
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3269/10
3269/50
SD 208 | CAS No. 627536-09-8 | TGF-beta Receptor Inhibitors
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Description: Potent ATP-competitive TGF-βRI inhibitor

Chemical Name: 2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine

Purity: ≥98%

Product Details
Citations (10)
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Biological Activity

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.

Technical Data

M.Wt:
352.75
Formula:
C17H10ClFN6
Solubility:
Soluble to 20 mM in DMSO with gentle warming
Purity:
≥98%
Storage:
Store at RT
CAS No:
627536-09-8

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.

Background References

  1. Transforming growth factor ?1-mediated functional inhibition of mesenchymal stromal cells in myelodysplastic syndromes and acute myeloid leukemia
    S Geyh, M Rodríguez-, P Jäger, A Koch, F Bormann, J Gutekunst, C Zilkens, U Germing, G Kobbe, F Lyko, R Haas, T Schroeder
    Haematologica, 2018;103(9):1462-1471.
  2. Bone marrow fibroblasts parallel multiple myeloma progression in patients and mice: in vitro and in vivo studies.
    Frassanito M, Rao L, Moschetta M, Ria R, di Marzo L, De Luisi A, Racanelli V, Catacchio I, Berardi S, Basile A, Menu E, Ruggieri S, Nico B, Ribatti D, Fumarulo R, Dammacco F, Vanderkerken K, Vacca A
    , 2014;0(0):.
  3. Unraveling the signaling pathways promoting fibrosis in Dupuytren's disease reveals TNF as a therapeutic target.
    Verjee L, Verhoekx J, Chan J, Krausgruber T, Nicolaidou V, Izadi D, Davidson D, Feldmann M, Midwood K, Nanchahal J
    Proc Natl Acad Sci U S A, 2013;110(10):E928-37.
  4. Protons sensitize epithelial cells to mesenchymal transition.
    Wang M, Hada M, Saha J, Sridharan D, Pluth J, Cucinotta F
    PLoS ONE, 2012;7(7):e41249.
  5. 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
  6. 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.
    Mol.Pharmacol., 2006;70:518
  7. 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.
    J.Pharmacol.Exp.Ther., 2006;319:586
  8. Inhibition of transforming growth factor-β attenuates brain injury and neurological deficits in a rat model of germinal matrix hemorrhage.
    Manaenko et al.
    Stroke, 2014;45:828

Product Datasheets

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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

  1. 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
  2. Transforming growth factor β1-mediated functional inhibition of mesenchymal stromal cells in myelodysplastic syndromes and acute myeloid leukemia.
    Authors: Geyh Et al.
    Haematologica  2018;103(9):1462
  3. The Wound Microenvironment Reprograms Schwann Cells to Invasive Mesenchymal-like Cells to Drive Peripheral Nerve Regeneration.
    Authors: Clements Et al.
    Neuron  2017;96:98
  4. 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
  5. MetF. inhibits proliferation and migration of glioblastoma cells independently of TGF-β2.
    Authors: Seliger Et al.
    Cell Cycle  2016;15:1755
  6. Protons sensitize epithelial cells to mesenchymal transition.
    Authors: Wang Et al.
    PLoS One  2012;7:e41249
  7. 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
  8. Transforming growth factor-β regulates the growth of valve interstitial cells in vitro.
    Authors: Li and Gotlieb
    Am J Pathol  2011;179:1746
  9. Hepcidin regulation by innate immune and infectious stimuli.
    Authors: Armitage Et al.
    Blood  2011;118:4129
  10. 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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