RG2833 是一种脑渗透性 HDAC 抑制剂，对 HDAC1 和 HDAC3 的 IC50 分别为 60 nM 和 50 nM，Ki值分别为 32 和 5 nM。

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

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.

1215493-56-3

C20H25N3O2

339.43

RGFP109

Ethanol:10 mg/mL (29.46 mM)
DMSO:63 mg/mL (185.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years