UK-5099

Last updated

UK-5099
UK-5099.svg
Clinical data
Other namesUK5099; JXL001; JXL-001; 2-Cyano-3-(1-phenylindol-3-yl)acrylate; 2-CPIYA
Drug class Mitochondrial pyruvate carrier (MPC) inhibitor
ATC code
  • None
Identifiers
  • (E)-2-cyano-3-(1-phenylindol-3-yl)prop-2-enoic acid
CAS Number
PubChem CID
ChemSpider
ChEBI
ChEMBL
Chemical and physical data
Formula C18H12N2O2
Molar mass 288.306 g·mol−1
3D model (JSmol)
  • C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)/C=C(\C#N)/C(=O)O
  • InChI=1S/C18H12N2O2/c19-11-13(18(21)22)10-14-12-20(15-6-2-1-3-7-15)17-9-5-4-8-16(14)17/h1-10,12H,(H,21,22)/b13-10+
  • Key:BIZNHCWFGNKBBZ-JLHYYAGUSA-N

UK-5099, also known as JXL001 or as 2-cyano-3-(1-phenylindol-3-yl)acrylate (2-CPIYA), is a mitochondrial pyruvate carrier (MPC) inhibitor. [1] It has been found to promote hair growth when administered topically to the skin in rodents. [2] [3] The drug was first described in the scientific literature by at least 1975. [4] [5] Analogues of UK-5099 like JXL069, JXL082, and PP405 have been developed. [2] [6] [7]

See also

References

  1. ↑ Tavoulari S, Sichrovsky M, Kunji ER (August 2023). "Fifty years of the mitochondrial pyruvate carrier: New insights into its structure, function, and inhibition". Acta Physiologica. 238 (4) e14016. doi:10.1111/apha.14016. PMC   10909473 . PMID   37366179.
  2. 1 2 Liu X, Flores AA, Situ L, Gu W, Ding H, Christofk HR, et al. (February 2021). "Development of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss". Journal of Medicinal Chemistry. 64 (4): 2046–2063. doi:10.1021/acs.jmedchem.0c01570. PMC   8939290 . PMID   33534563.
  3. ↑ Flores A, Schell J, Krall AS, Jelinek D, Miranda M, Grigorian M, et al. (September 2017). "Lactate dehydrogenase activity drives hair follicle stem cell activation". Nature Cell Biology. 19 (9): 1017–1026. doi:10.1038/ncb3575. PMC   5657543 . PMID   28812580.
  4. ↑ Halestrap AP (April 1975). "The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors". The Biochemical Journal. 148 (1): 85–96. doi:10.1042/bj1480085. PMC   1165509 . PMID   1156402.
  5. ↑ Halestrap AP, Denton RM (April 1975). "The specificity and metabolic implications of the inhibition of pyruvate transport in isolated mitochondria and intact tissue preparations by alpha-Cyano-4-hydroxycinnamate and related compounds". The Biochemical Journal. 148 (1): 97–106. doi:10.1042/bj1480097. PMC   1165510 . PMID   1171687.
  6. ↑ Brown L (12 August 2025). "The Great Unbalding Draws Nearer". Intelligencer. Retrieved 23 October 2025.
  7. ↑ Huang Y, Peng X, Zhang H, Pan M, Su X, Li G, et al. (November 2024). "Design, synthesis and biological evaluation of novel cyano-cinnamate derivatives as mitochondrial pyruvate carrier inhibitors". Bioorganic & Medicinal Chemistry Letters. 112 129923. doi:10.1016/j.bmcl.2024.129923. PMID   39134097.
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