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Submit ReviewSB 525334 is a selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). Inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells. Attenuates bleomycin-induced pulmonary fibrosis.
Sold with the permission of GlaxoSmithKline
SB 525334 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。
分子量 | 343.42 |
公式 | C21H21N5 |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 356559-20-1 |
PubChem ID | 9967941 |
InChI Key | DKPQHFZUICCZHF-UHFFFAOYSA-N |
Smiles | CC1=NC(C4=C(NC(C(C)(C)C)=N4)C2=CC=C(N=CC=N3)C3=C2)=CC=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 34.34 | 100 |
以下数据基于产品分子量 343.42。 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 |
---|---|---|---|
1 mM | 2.91 mL | 14.56 mL | 29.12 mL |
5 mM | 0.58 mL | 2.91 mL | 5.82 mL |
10 mM | 0.29 mL | 1.46 mL | 2.91 mL |
50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
参考文献是支持产品生物活性的出版物。
Grygielko et al (2005) Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-β type I receptor kinase in puromycin-induced nephritis. J.Pharmacol.Exp.Ther. 313 943 PMID: 15769863
Higashiyama et al (2007) Inhibition of AVNreceptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis Exp.Mol.Pathol. 83 39 PMID: 17274978
Laping et al (2007) Tumor-specific efficacy of transforming growth factor-βRI inhibition in eker rats. Clin.Cancer Res. 13 3087 PMID: 17505012
If you know of a relevant reference for SB 525334, please let us know.
关键词: SB 525334, SB 525334 supplier, Selective, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1Transforming, Growth, Factors, Beta, Receptors, TGF-beta, Receptor, Serine/Threonine, Kinases, RSTKs, SB525334, GlaxoSmithKline, GSK, 3211, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SB 525334 的部分引用包括:
Ng et al (2012) Progenitor-like traits contribute to patient survival and prognosis in oligodendroglial tumors. Clin Cancer Res 18 4122 PMID: 22675171
Denby et al (2014) MicroRNA-214 antagonism protects against renal fibrosis. J Am Soc Nephrol 25 65 PMID: 24158985
Kleczko et al (2015) An Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases. PLoS One 10 e0123600 PMID: 25946135
Gutiérrez et al (2015) RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice. Lab Chip 10 e0135005 PMID: 26247610
Grygielewicz et al (2014) Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells. Gastric Cancer PMID: 25407459
Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. Sci Rep 13 1969 PMID: 23563587
Kilari et al (2018) Increased transforming growth factor beta (TGF-β) and pSMAD3 signaling in a Murine Model for Contrast Induced Kidney Injury. Sci Rep 8 6630 PMID: 29700311
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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。
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.