Description
RG2833 is a brain-penetrant inhibitor of HDAC with IC50 values of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
Product Overview
RG2833 is a histone deacetylase (HDAC) inhibitor. In the neuronal cell, RG2833 increased Friedreich Ataxia (FXN) mRNA and protein levels, with concomitant changes in the epigenetic state of the gene. In PBMCs, RG2833 inhibited HDAC expression and increased H3K9 acetylation, and increased FXN mRNA in blood from patients. In iPSC-derived neuronal cell model, plasma RG2833 (5μM) inhibited maximal deacetylase and upregulated FXN. The result showed a good correlation between increase in FXN transcript and inhibition of deacetylase activity, providing evidence that the mechanism of action of RG2833 is through deacetylation.
Synonyms
RG 2833; RG-2833; RGFP-109; RGFP109; RGFP 109
Molecular Formula
C20H25N3O2
Chemical Name
N-[6-(2-aminoanilino)-6-oxohexyl]-4-methylbenzamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request