RG2833 (RGFP109) (RGFP109), a brain-penetrant HDAC inhibitor, is with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.

HDAC1:32 nM(Ki), HDAC3:5 nM(Ki)

In unstimulated peripheral blood mononuclear cells, RG2833 upregulates the level of the synaptic mRNA and protein in a dose-dependent manner.

Aconitase activities are determined by homogenization of mouse brain tissues on ice at 10% w/v in CellLytic MT Mammalian Tissue Lysis/Extraction buffer, followed by centrifugation at 800×g?for 10?min at 4°C. Tissue lysates (50?μL) are then added to 200?μL of substrate mix (50?mM Tris/HCl pH 7.4, 0.4?mM NADP, 5?mM Na citrate, 0.6?mM MgCl2, 0.1% (v/v) Triton X-100 and 1U isocitrate dehydrogenase) and the reactions are incubated at 37°C for 15?min, followed by spectrophotometric absorbance measurements every minute for 15?min at 340?nm 37°C to determine the reaction slope. Aconitase activities of mouse brain tissues are then normalized to citrate synthase activities, which are determined using a citrate synthase assay kit.