SB-431542

Last updated
SB-431542
SB431542.svg
Names
Preferred IUPAC name
4-[4-(2H-1,3-Benzodioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl]benzamide
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
PubChem CID
UNII
  • InChI=1S/C22H16N4O3/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17/h1-11H,12H2,(H2,23,27)(H,25,26)
    Key: FHYUGAJXYORMHI-UHFFFAOYSA-N
  • InChI=1/C22H16N4O3/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17/h1-11H,12H2,(H2,23,27)(H,25,26)
    Key: FHYUGAJXYORMHI-UHFFFAOYAN
  • NC(=O)c1ccc(cc1)c2nc(c3ccc4OCOc4c3)c([nH]2)c5ccccn5
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).

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] SB431542 can also be used in combination with LDN193189, CHIR99021 and DAPT to transform astrocytes into neurons. [2] 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. [3]

References

  1. 1 2 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. ↑ 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. 12 (3): 488–501. doi:10.1016/j.stemcr.2019.01.003. PMC   6409415 . PMID   30745031.
  3. ↑ Mondanelli G; Bianchi R; Pallotta MT; Orabona C; Albini E; Iacono A; Belladonna ML; Vacca C; Fallarino F; Macchiarulo A; Ugel S; Bronte V; Gevi F; Zolla L; Verhaar A; Peppelenbosch M; Mazza EMC; Bicciato S; Laouar Y; Santambrogio L; Puccetti P; Volpi C; Grohmann U (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 . PMC   5337620 . PMID   30745031.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.