SB-431542

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).

SB-431542
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
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).
Infobox references

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]

gollark: (they aren't, I think)
gollark: Trouble is that it's slow, so presumably if they did there'd be periodic lag as they updated all their dragons.
gollark: I wonder how hatcheries update their stuff. Is it just periodic or something else?
gollark: Or granduncle or whatever.
gollark: I think I have one which is a great uncle of that

References

  1. Laping, NJ; Grygielko E; Mathur A; Butter S; Bomberger J; Tweed C; Martin W; Fornwald J; Lehr R; Harling J; Gaster L; Callahan JF; Olson BA (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.
  2. 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. PMC 3659681. PMID 23197756.
  3. Yin, Jiu-Chao; Zhang, Lei; Ma, Ning-Xin; Wang, Yue; Lee, Grace; Hou, Xiao-Yi; Lei, Zhuo-Fan; Zhang, Feng-Yu; Dong, Feng-Ping; Wu, Gang-Yi; Chen, Gong (2019). "Chemical Conversion of Human Fetal Astrocytes into Neurons through Modulation of Multiple Signaling Pathways". Stem Cell Reports. doi:10.1016/j.stemcr.2019.01.003. PMC 6409415. PMID 30745031.
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