Crebinostat

Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC₅₀ values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice^[1]. In Vitro: Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells^[1].
Crebinostat (1 μM; 24 h) downregulates Mapt mRNA expression, and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression in mouse primary cultured neurons^[1].
Crebinostat (1 μM; 24 h) increases histone acetylation and synapsin I punctae along dendrites in primary cultured neurons^[1]. In Vivo: Crebinostat (25 mg/kg; IP; for 10 days) enhances memory of contextual fear conditioning in mice; induces an increase in total hippocampal acetylation of H4K12 and H3K9^[1].