Chemistry:RGFP963

From HandWiki

RGFP963, or RGFP-963, is a histone deacetylase (HDAC) inhibitor which is used in scientific research.[1][2][3][4][5] It is a selective class I HDAC inhibitor, including of HDAC1, HDAC2, and HDAC3 (IC50 = 1,510 nM, 750 nM, and 96 nM, respectively).[1][2] The drug also weakly inhibits HDAC10 (IC50 = 6,640–10,000 nM), whereas it showed no inhibition of other HDACs at a concentration of up to 20,000 nM.[1][2] RGFP963 enhances the consolidation of cued fear extinction in rodents, with this thought to be mediated by inhibition of HDAC1 and/or HDAC2 and not by inhibition of HDAC3.[1][4] In addition, the drug promotes synaptogenesis in vitro and enhances memory in an animal model of Alzheimer's disease in rodents.[2][4][6] It also enhanced cognition in a model of amyotrophic lateral sclerosis (ALS) in rodents.[3] The pharmacokinetics of RGFP963 have been studied and it is brain-penetrant in rodents.[1] RGFP963 was first described in the scientific literature by 2015.[1][2]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "The Class I HDAC inhibitor RGFP963 enhances consolidation of cued fear extinction". Learning & Memory (Cold Spring Harbor, N.Y.) 22 (4): 225–231. April 2015. doi:10.1101/lm.036699.114. PMID 25776040. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "Pharmacological Selectivity Within Class I Histone Deacetylases Predicts Effects on Synaptic Function and Memory Rescue". Neuropsychopharmacology 40 (10): 2307–2316. September 2015. doi:10.1038/npp.2015.93. PMID 25837283. 
  3. ↑ 3.0 3.1 "Reversal of cognitive deficits in FUSR521G amyotrophic lateral sclerosis mice by arimoclomol and a class I histone deacetylase inhibitor independent of heat shock protein induction". Neurotherapeutics 21 (5). September 2024. doi:10.1016/j.neurot.2024.e00388. PMID 38972779. 
  4. ↑ 4.0 4.1 4.2 "Histone Deacetylase (HDAC) Inhibitors - emerging roles in neuronal memory, learning, synaptic plasticity and neural regeneration". Current Neuropharmacology 14 (1): 55–71. 2016. doi:10.2174/1570159x13666151021111609. PMID 26487502. 
  5. ↑ "Delving into the Latest Updates on RGFP-963 with Synapse". 7 March 2026. https://synapse.patsnap.com/drug/d8645203e9fd4a37a1d581b61d9d86cf. 
  6. ↑ "The development prospection of HDAC inhibitors as a potential therapeutic direction in Alzheimer's disease". Translational Neurodegeneration 6. 2017. doi:10.1186/s40035-017-0089-1. PMID 28702178. 



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