IU1

Last updated

IU1
IU1 structure.png
Identifiers
  • 1-[1-(4-fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-pyrrolidin-1-ylethanone
CAS Number
PubChem CID
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C18H21FN2O
Molar mass 300.377 g·mol−1
3D model (JSmol)
  • CC1=CC(=C(N1C2=CC=C(C=C2)F)C)C(=O)CN3CCCC3
  • InChI=1S/C18H21FN2O/c1-13-11-17(18(22)12-20-9-3-4-10-20)14(2)21(13)16-7-5-15(19)6-8-16/h5-8,11H,3-4,9-10,12H2,1-2H3
  • Key:JUWDSDKJBMFLHE-UHFFFAOYSA-N

IU1 is a drug used in scientific research which acts as a selective inhibitor of the ubiquitin-specific processing protease enzyme USP14. [1] It is of interest in anti-cancer and antiviral research and also as a potential anti-aging drug. Numerous derivatives of IU1 have been developed with up to 10x the potency of IU1 as USP14 inhibitors, [2] [3] but IU1 remains the most widely used compound in research in this area. [4] [5] [6] [7] [8] [9] [10]

References

  1. ↑ Lee BH, Lee MJ, Park S, Oh DC, Elsasser S, Chen PC, et al. (September 2010). "Enhancement of proteasome activity by a small-molecule inhibitor of USP14". Nature. 467 (7312): 179–84. Bibcode:2010Natur.467..179L. doi:10.1038/nature09299. PMC   2939003 . PMID   20829789.
  2. ↑ Wang Y, Jiang Y, Ding S, Li J, Song N, Ren Y, et al. (December 2018). "Small molecule inhibitors reveal allosteric regulation of USP14 via steric blockade". Cell Research. 28 (12): 1186–1194. doi:10.1038/s41422-018-0091-x. PMC   6274642 . PMID   30254335.
  3. ↑ Boselli M, Lee BH, Robert J, Prado MA, Min SW, Cheng C, et al. (November 2017). "An inhibitor of the proteasomal deubiquitinating enzyme USP14 induces tau elimination in cultured neurons". The Journal of Biological Chemistry. 292 (47): 19209–19225. doi: 10.1074/jbc.M117.815126 . PMC   5702663 . PMID   28972160.
  4. ↑ Nag DK, Finley D (April 2012). "A small-molecule inhibitor of deubiquitinating enzyme USP14 inhibits Dengue virus replication". Virus Research. 165 (1): 103–106. doi:10.1016/j.virusres.2012.01.009. PMID   22306365.
  5. ↑ Moon S, Muniyappan S, Lee SB, Lee BH (June 2021). "Small-Molecule Inhibitors Targeting Proteasome-Associated Deubiquitinases". International Journal of Molecular Sciences. 22 (12): 6213. doi: 10.3390/ijms22126213 . PMC   8226605 . PMID   34207520.
  6. ↑ Wang F, Ning S, Yu B, Wang Y (2022). "USP14: Structure, Function, and Target Inhibition". Frontiers in Pharmacology. 12 801328. doi: 10.3389/fphar.2021.801328 . PMC   8766727 . PMID   35069211.
  7. ↑ Pan J, Zhao J, Feng L, Xu X, He Z, Liang W (March 2023). "Inhibition of USP14 Suppresses ROS-dependent Ferroptosis and Alleviates Renal Ischemia/Reperfusion Injury". Cell Biochemistry and Biophysics. 81 (1): 87–96. doi:10.1007/s12013-022-01107-y. PMID   36255562.
  8. ↑ Hou W, Yao J, Liu J, Lin X, Wei J, Yin X, et al. (November 2023). "USP14 inhibition promotes recovery by protecting BBB integrity and attenuating neuroinflammation in MCAO mice". CNS Neuroscience & Therapeutics. 29 (11): 3612–3623. doi:10.1111/cns.14292. PMC   10580339 . PMID   37269080.
  9. ↑ Lim JJ, Noh S, Kang W, Hyun B, Lee BH, Hyun S (December 2024). "Pharmacological inhibition of USP14 delays proteostasis-associated aging in a proteasome-dependent but foxo-independent manner". Autophagy. 20 (12): 2752–2768. doi:10.1080/15548627.2024.2389607. PMC   11587835 . PMID   39113571.
  10. ↑ Zhou X, Xia Q, Wang B, Li J, Liu B, Wang S, et al. (2025). "USP14 modulates stem-like properties, tumorigenicity, and radiotherapy resistance in glioblastoma stem cells through stabilization of MST4-phosphorylated ALKBH5". Theranostics. 15 (6): 2293–2314. doi:10.7150/thno.103629. PMC   11840735 . PMID   39990235.


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