Selisistat

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Selisistat
Selisistat.svg
Identifiers
  • 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.190.284 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C13H13ClN2O
Molar mass 248.71 g·mol−1
3D model (JSmol)
  • C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N
  • InChI=1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)
  • Key:FUZYTVDVLBBXDL-UHFFFAOYSA-N

Selisistat (EX-527) is an experimental drug which is a potent and selective inhibitor of the SIRT1 protein. It was developed as a potential agent for the treatment of Huntington's disease, but also has potential applications in cancer treatment. [1] [2] [3] [4] [5]

References

  1. ↑ Kulkarni P, Saxena U (December 2014). "Investigational drugs for the management of Huntington's disease: are we there yet?". Expert Opinion on Investigational Drugs. 23 (12): 1595–1603. doi:10.1517/13543784.2014.934807. PMID   25084527.
  2. ↑ Shannon KM, Fraint A (September 2015). "Therapeutic advances in Huntington's Disease". Movement Disorders. 30 (11): 1539–1546. doi:10.1002/mds.26331. PMID   26226924.
  3. ↑ Bai X, Yao L, Ma X, Xu X (2018). "Small Molecules as SIRT Modulators". Mini Reviews in Medicinal Chemistry. 18 (13): 1151–1157. doi:10.2174/1389557516666160620095103. PMID   27334466.
  4. ↑ Guo R, Wei Y, Du Y, Liu L, Zhang H, Ren R, et al. (December 2024). "EX527, a sirtuins 1 inhibitor, sensitizes T-cell leukemia to death receptor-mediated apoptosis by downregulating cellular FLICE inhibitory protein". Cancer Biology & Therapy. 25 (1) 2402588. doi:10.1080/15384047.2024.2402588. PMC   11409494 . PMID   39286953.
  5. ↑ Wawruszak A, Luszczki J, Bartuzi D, Kalafut J, Okon E, Czerwonka A, et al. (December 2025). "Selisistat, a SIRT1 inhibitor, enhances paclitaxel activity in luminal and triple-negative breast cancer: in silico, in vitro, and in vivo studies". Journal of Enzyme Inhibition and Medicinal Chemistry. 40 (1) 2458554. doi:10.1080/14756366.2025.2458554. PMC   11823383 . PMID   39935420.
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