RGFP963

RGFP963

RGFP963
Clinical data
Other namesRGFP-963
Drug classHistone deacetylase inhibitor; HDAC1, HDAC2, and HDAC3 inhibitor; Cognitive enhancer
ATC code
  • None
Identifiers
  • (E)-N-(2-aminophenyl)-3-[1-[(E)-3-phenylprop-2-enyl]pyrazol-4-yl]prop-2-enamide
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC21H20N4O
Molar mass344.418 g·mol−1
3D model (JSmol)
  • C1=CC=C(C=C1)/C=C/CN2C=C(C=N2)/C=C/C(=O)NC3=CC=CC=C3N
  • InChI=1S/C21H20N4O/c22-19-10-4-5-11-20(19)24-21(26)13-12-18-15-23-25(16-18)14-6-9-17-7-2-1-3-8-17/h1-13,15-16H,14,22H2,(H,24,26)/b9-6+,13-12+
  • Key:KOESHVZEHKMOIK-UXKPLKHMSA-N
RGFP963 activities
Enzyme IC50Tooltip Half-maximal inhibitory concentration (nM)
HDAC1 1,510
HDAC2 750
HDAC3 96
HDAC4 >20,000
HDAC5 >20,000
HDAC6 >20,000
HDAC7 >20,000
HDAC8 >20,000
HDAC9 >20,000
HDAC10 6,640–10,000
HDAC11 27,700
Refs: [1][2]

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 (IC50Tooltip half-maximal inhibitory concentration = 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. ^ a b c d e f g Bowers ME, Xia B, Carreiro S, Ressler KJ (April 2015). "The Class I HDAC inhibitor RGFP963 enhances consolidation of cued fear extinction". Learning & Memory. 22 (4). Cold Spring Harbor, N.Y.: 225–231. doi:10.1101/lm.036699.114. PMC 4371170. PMID 25776040.
  2. ^ a b c d e f Rumbaugh G, Daws SE, Ozkan ED, Rojas CS, Hubbs CR, Aceti M, et al. (September 2015). "Pharmacological Selectivity Within Class I Histone Deacetylases Predicts Effects on Synaptic Function and Memory Rescue". Neuropsychopharmacology. 40 (10): 2307–2316. doi:10.1038/npp.2015.93. PMC 4538358. PMID 25837283.
  3. ^ a b Pelaez MC, Fiore F, Larochelle N, Dabbaghizadeh A, Comaduran MF, Arbour D, et al. (September 2024). "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) e00388. doi:10.1016/j.neurot.2024.e00388. PMC 11579874. PMID 38972779.
  4. ^ a b c Ganai SA, Ramadoss M, Mahadevan V (2016). "Histone Deacetylase (HDAC) Inhibitors - emerging roles in neuronal memory, learning, synaptic plasticity and neural regeneration". Current Neuropharmacology. 14 (1): 55–71. doi:10.2174/1570159x13666151021111609. PMC 4787286. PMID 26487502.
  5. ^ "Delving into the Latest Updates on RGFP-963 with Synapse". Synapse. 7 March 2026. Retrieved 6 August 2026.
  6. ^ Yang SS, Zhang R, Wang G, Zhang YF (2017). "The development prospection of HDAC inhibitors as a potential therapeutic direction in Alzheimer's disease". Translational Neurodegeneration. 6 19. doi:10.1186/s40035-017-0089-1. PMC 5504819. PMID 28702178.

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