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Submit ReviewSD 208
说明： Potent ATP-competitive TGF-βRI inhibitor
化学名： 2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for SD 208
SD 208 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for SD 208
| 分子量 | 352.75 |
| 公式 | C17H10ClFN6 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SD 208
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 7.05 | 20 温和加热 |
制备储备液 for SD 208
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for SD 208
参考文献 for SD 208
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 SD 208 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SD 208 的部分引用包括：
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Stem Cell Research Product Guide
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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 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 SD 208
