Crebinostat is a histone deacetylase (HDAC) inhibitor and possible cognitive enhancer.
Pharmacology + Enzyme (nM) HDAC1 0.7–1.4 HDAC2 1.0–2.1 HDAC3 2.0–3.4 HDAC4 >2,000 HDAC5 >2,000 HDAC6 0.6–9.3 HDAC7 >2,000 HDAC8 >2,000 HDAC9 >2,000 HDAC10 HDAC11 Refs:
Crebinostat is a histone deacetylase (HDAC) inhibitor, specifically inhibiting the class I HDAC1, HDAC2, and HDAC3, the class IIb HDAC6, and weakly the class I HDAC8, with no significant inhibition of the class IIa HDAC4, HDAC5, HDAC7, or HDAC9. The drug has been found to robustly activate CREB-mediated transcription and to upregulate brain-derived neurotrophic factor (BDNF) expression and increase synaptogenesis. It has been found to enhance memory in rodents. The pharmacokinetics of crebinostat have been studied in rodents.
Chemistry The chemical synthesis of crebinostat has been described. A notable analogue of crebinostat is neurinostat.
History Crebinostat was first described in the scientific literature by 2013. It was identified via screening of a library of over 1,200compounds designed to target HDACs. There is interest in crebinostat as a potential novel cognitive enhancer in humans. Subsequent to the development of crebinostat, an analogue known as neurinostat with improved properties was discovered and described.
See also Histone deacetylase inhibitor Synapsinostat Neurinostat Vorinostat
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