H-151

H-151
Identifiers
  • 1-(4-ethylphenyl)-3-(1H-indol-3-yl)urea
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H17N3O
Molar mass279.343 g·mol−1
3D model (JSmol)
  • CCC1=CC=C(C=C1)NC(=O)NC2=CNC3=CC=CC=C32
  • InChI=1S/C17H17N3O/c1-2-12-7-9-13(10-8-12)19-17(21)20-16-11-18-15-6-4-3-5-14(15)16/h3-11,18H,2H2,1H3,(H2,19,20,21)
  • Key:UJZDIKVQFMCLBE-UHFFFAOYSA-N

H-151 is an experimental drug which acts as an irreversible antagonist of the stimulator of interferon genes (STING) protein. It has antiinflammatory and antiviral effects by reducing cytokine signalling, and has potential application in numerous disease states in which inflammation plays a role.[1][2][3][4][5][6][7][8][9][10][11]

See also

References

  1. ^ Haag SM, Gulen MF, Reymond L, Gibelin A, Abrami L, Decout A, et al. (July 2018). "Targeting STING with covalent small-molecule inhibitors". Nature. 559 (7713): 269–273. Bibcode:2018Natur.559..269H. doi:10.1038/s41586-018-0287-8. PMID 29973723.
  2. ^ Liu Y, Lu X, Qin N, Qiao Y, Xing S, Liu W, et al. (February 2021). "STING, a promising target for small molecular immune modulator: A review". European Journal of Medicinal Chemistry. 211 113113. doi:10.1016/j.ejmech.2020.113113. PMID 33360799.
  3. ^ Domizio JD, Gulen MF, Saidoune F, Thacker VV, Yatim A, Sharma K, et al. (March 2022). "The cGAS-STING pathway drives type I IFN immunopathology in COVID-19". Nature. 603 (7899): 145–151. Bibcode:2022Natur.603..145D. doi:10.1038/s41586-022-04421-w. PMC 8891013. PMID 35045565.
  4. ^ Kobritz M, Borjas T, Patel V, Coppa G, Aziz M, Wang P (September 2022). "H151, A Small Molecule Inhibitor of Sting as a Novel Therapeutic in Intestinal Ischemia-Reperfusion Injury". Shock. 58 (3): 241–250. doi:10.1097/SHK.0000000000001968. PMC 9489661. PMID 35959789.
  5. ^ Zhao J, Xiao R, Zeng R, He E, Zhang A (August 2022). "Small molecules targeting cGAS-STING pathway for autoimmune disease". European Journal of Medicinal Chemistry. 238 114480. doi:10.1016/j.ejmech.2022.114480. PMID 35635952.
  6. ^ Wu G, Zhang Y, Niu L, Hu Y, Yang Y, Zhao Y (May 2024). "Interleukin-1β promotes human metapneumovirus replication via activating the cGAS-STING pathway". Virus Research. 343 199344. doi:10.1016/j.virusres.2024.199344. PMC 10982080. PMID 38431054.
  7. ^ Tanaka M, Yasuda H, Nakamura S, Shimazawa M (July 2024). "H-151, a Selective STING Inhibitor, Has Potential as a Treatment for Neovascular Age-Related Macular Degeneration". Investigative Ophthalmology & Visual Science. 65 (8): 16. doi:10.1167/iovs.65.8.16. PMC 11235146. PMID 38980271.
  8. ^ Ge X, Liu Q, Fan H, Yu H, Li J, Li Y, et al. (November 2024). "STING facilitates the development of radiation-induced lung injury via regulating the PERK/eIF2α pathway". Translational Lung Cancer Research. 13 (11): 3010–3025. doi:10.21037/tlcr-24-649. PMC 11632424. PMID 39670000.
  9. ^ Xia L, Jiang JH, Liu JY, Zhang TY, Dong YX, Liu QH, et al. (December 2024). "H-151 attenuates lipopolysaccharide-induced acute kidney injury by inhibiting the STING-TBK1 pathway". Renal Failure. 46 (2) 2363591. doi:10.1080/0886022X.2024.2363591. PMC 11168233. PMID 38856314.
  10. ^ Liu Z, Qin Q, Wang S, Kang X, Liu Y, Wei L, et al. (December 2024). "STING Activation in Macrophages and Microglia Drives Poststroke Inflammation: Implications for Neuroinflammatory Mechanisms and Therapeutic Interventions". CNS Neuroscience & Therapeutics. 30 (12) e70106. doi:10.1111/cns.70106. PMC 11656094. PMID 39698742.
  11. ^ Sun Y, Zou S, Xu X, Xu S, Sun H, Tang M, et al. (March 2025). "Inhibition of the cGAS‑STING Pathway Reduces Cisplatin-Induced Inner Ear Hair Cell Damage". Neuroscience Bulletin. 41 (3): 359–373. doi:10.1007/s12264-024-01334-8. PMC 11876498. PMID 39676140.

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