// Workers AI · dad joke modeWhat did RGFP963 say to its date? You're a gene-ius match
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| Clinical data | |
|---|---|
| Other names | RGFP-963 |
| Drug class | Histone deacetylase inhibitor; HDAC1, HDAC2, and HDAC3 inhibitor; Cognitive enhancer |
| ATC code |
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| Identifiers | |
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| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C21H20N4O |
| Molar mass | 344.418 g·mol−1 |
| 3D model (JSmol) | |
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| Enzyme | IC50 (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 (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
[edit]References
[edit]- 1 2 3 4 5 6 7 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.
- 1 2 3 4 5 6 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.
- 1 2 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.
- 1 2 3 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.
- ↑ "Delving into the Latest Updates on RGFP-963 with Synapse". Synapse. 7 March 2026. Retrieved 6 August 2026.
- ↑ 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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