| Description |
RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively. |
| Features |
Orally bioavailable, HDAC inhibitor that penetrates into brain tissue. |
|
Targets
|
HDAC3 [1]
(Cell-free assay) |
HDAC1 [1]
(Cell-free assay) |
HDAC3 [1]
(Cell-free assay) |
HDAC1 [1]
(Cell-free assay) |
| 5 nM(Ki) |
32 nM(Ki) |
5 nM(Ki) |
32 nM(Ki) |
|
| In vitro |
RGFP109 dose-dependently upregulates frataxin mRNA and protein levels in cultures of unstimulated peripheral blood mononuclear cells (PBMC) obtained from FRDA patients. [1]
|
| In vivo |
RG2833 (150 mg/kg) corrects frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice without acute toxicity signs. [1] RGFP109 ameliorates the disease phenotype of a Friedreich ataxia mouse model. [2] RGFP109 (30 mg/kg p.o.) also alleviates established l-DOPA-induced dyskinesia. [3]
|
COA
HPLC