Degrasyn

Last updated
Degrasyn
WP1130 structure.png
Identifiers
  • (E)-3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]prop-2-enamide
CAS Number
PubChem CID
CompTox Dashboard (EPA)
Chemical and physical data
Formula C19H18BrN3O
Molar mass 384.277 g·mol−1
3D model (JSmol)
  • CCC[C@@H](C1=CC=CC=C1)NC(=O)/C(=C/C2=NC(=CC=C2)Br)/C#N
  • InChI=1S/C19H18BrN3O/c1-2-7-17(14-8-4-3-5-9-14)23-19(24)15(13-21)12-16-10-6-11-18(20)22-16/h3-6,8-12,17H,2,7H2,1H3,(H,23,24)/b15-12+/t17-/m0/s1
  • Key:LIDOPKHSVQTSJY-VMEIHUARSA-N

Degrasyn (WP1130) is a drug used in scientific research which acts as a non-selective inhibitor of proteasome deubiquitinases. It has antiviral properties, and potential applications in the treatment of cancer. [1] [2] [3] [4] [5]

References

  1. ↑ Kapuria V, Peterson LF, Fang D, Bornmann WG, Talpaz M, Donato NJ (November 2010). "Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis". Cancer Research. 70 (22): 9265–9276. doi:10.1158/0008-5472.CAN-10-1530. PMID   21045142.
  2. ↑ Ning F, Xin H, Liu J, Lv C, Xu X, Wang M, et al. (July 2020). "Structure and function of USP5: Insight into physiological and pathophysiological roles". Pharmacological Research. 157 104557. doi:10.1016/j.phrs.2019.104557. PMID   31756387.
  3. ↑ López LS, Calvo EP, Castellanos JE (February 2023). "Deubiquitinating Enzyme Inhibitors Block Chikungunya Virus Replication". Viruses. 15 (2): 481. doi: 10.3390/v15020481 . PMC   9966916 . PMID   36851696.
  4. ↑ Wang J, Fang S, Jiang Y, Hua Q (2024). "Unraveling the Mechanism of Action of Ubiquitin-Specific Protease 5 and Its Inhibitors in Tumors". Clinical Medicine Insights. Oncology. 18 11795549241281932. doi:10.1177/11795549241281932. PMC   11465303 . PMID   39391229.
  5. ↑ Oak S, Karajgikar O, Gadewal N, Sulkshane P, Verma T, Gupta S, Teni T (June 2025). "The deubiquitinase inhibitor WP1130 drives nuclear aggregation and reactivation of mutant p53 for selective cancer cell targeting". The FEBS Journal. 292 (11): 2823–2842. doi:10.1111/febs.70036. PMC   12138167 . PMID   40070163.
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