RG2833 (RGFP109) 1215493-56-3

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Molecular Weight:

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


Biological Activity


RGFP109 dose-dependently upregulates frataxin mRNA and protein levels in
cultures of unstimulated peripheral blood mononuclear cells (PBMC)
obtained from FRDA patients.


RG2833 (150 mg/kg) corrects frataxin deficiency and increases histone
acetylation in the brain and heart of KIKI mice without acute toxicity
signs. RGFP109 ameliorates the disease phenotype of a Friedreich ataxia mouse model. RGFP109 (30 mg/kg p.o.) also alleviates established l-DOPA-induced dyskinesia.


Time dependent IC50 value with pre-incubation


Deacetylation assays are based on the homogenous fluorescence release
assay. In brief, purified recombinant enzymes are incubated with
serial-diluted Inhibitors at various concentrations, with pre-incubation
times ranging from 0 to 3 hours, in the standard HDAC buffer.


Acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both
HDAC1 and HDAC3) is added after the pre-incubation period. The
reaction is allowed to run for 1 hour. The trypsin peptidase developer,
at final concentration of 5mg/ml, is added after 1 hour, and the
fluorescence emission is then measured using a Tecan M200 96-well plate
reader.

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Product Categories : Epigenetics > HDAC Inhibitor