Chemistry:SB-431542
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| Preferred IUPAC name
4-[4-(2H-1,3-Benzodioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl]benzamide | |
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3D model (JSmol)
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| Properties | |
| C22H16N4O3 | |
| Molar mass | 384.395 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
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SB-431542 is a drug candidate developed by GlaxoSmithKline (GSK) as an inhibitor of the activin receptor-like kinase (ALK) receptors, ALK5, ALK4 and ALK7.[1] However, it is not an inhibitor of anaplastic lymphoma kinase (which are commonly known as ALK inhibitors).
In-vitro studies
While SB-431542 has not proved directly useful for any clinical application, it is used for several applications in molecular biology. It suppresses the TGF-beta-induced proliferation of osteosarcoma cells in humans.[1] Treatment with SB431542 is a robust, clinically applicable, and efficient system for generating mesenchymal stem/stromal cells (MSCs) from human iPSCs.[2] SB431542 can also be used in combination with LDN193189, CHIR99021 and DAPT to transform astrocytes into neurons.[3] It is also commonly used for immunological studies, for instance as a TGF-β inhibitor to facilitate the generation of dendritic cells from peripheral blood monocytes. [4]
References
- ↑ 1.0 1.1 Laping, NJ; Grygielko E; Mathur A; Butter S; Bomberger J; Tweed C; Martin W; Fornwald J et al. (2002). "Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542". Molecular Pharmacology 62 (1): 58–64. doi:10.1124/mol.62.1.58. PMID 12065755.
- ↑ Chen, Yen Shun; Pelekanos, Rebecca A.; Ellis, Rebecca L.; Horne, Rachel; Wolvetang, Ernst J.; Fisk, Nicholas M. (2012). "Small Molecule Mesengenic Induction of Human Induced Pluripotent Stem Cells to Generate Mesenchymal Stem/Stromal Cells". Stem Cells Translational Medicine 1 (2): 83–95. doi:10.5966/sctm.2011-0022. PMID 23197756.
- ↑ Yin, Jiu-Chao; Zhang, Lei; Ma, Ning-Xin; Wang, Yue; Lee, Grace; Hou, Xiao-Yi; Lei, Zhuo-Fan; Zhang, Feng-Yu et al. (2019). "Chemical Conversion of Human Fetal Astrocytes into Neurons through Modulation of Multiple Signaling Pathways". Stem Cell Reports 12 (3): 488–501. doi:10.1016/j.stemcr.2019.01.003. PMID 30745031.
- ↑ Mondanelli G; Bianchi R; Pallotta MT; Orabona C; Albini E; Iacono A; Belladonna ML; Vacca C et al. (2017). "A Relay Pathway between Arginine and Tryptophan Metabolism Confers Immunosuppressive Properties on Dendritic Cells". Immunity 42 (2): 233–244. doi:10.1016/j.immuni.2017.01.005. PMID 30745031.
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