Name | RG2833 |
Synonyms | RG2833 RG 2833 RGFP109 RG-2833 RGFP 109 RGFP-109 RG2833(RGFP109) RGFP 109 N-[6-(2-Aminophenylamino)-6-oxohexyl]-4-methylbenzamide |
CAS | 1215493-56-3 |
Molecular Formula | C20H25N3O2 |
Molar Mass | 339.43 |
Density | 1.163±0.06 g/cm3(Predicted) |
Boling Point | 620.1±50.0 °C(Predicted) |
pKa | 14.62±0.70(Predicted) |
Storage Condition | -20℃ |
In vitro study | In unstimulated peripheral blood mononuclear cell (PBMC) medium, RGFP109 dose-dependently upregulated fraxin mRNA and protein levels. |
In vivo study | RG2833 (150 mg/kg) modulates frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice without signs of acute toxicity. RGFP109 improves disease phenotype in Friedreich ataxia mouse model. RGFP109 (30 mg/kg, oral) also alleviated established l-DOPA-induced dyskinesia. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.946 ml | 14.731 ml | 29.461 ml |
5 mM | 0.589 ml | 2.946 ml | 5.892 ml |
10 mM | 0.295 ml | 1.473 ml | 2.946 ml |
5 mM | 0.059 ml | 0.295 ml | 0.589 ml |
biological activity | RG2833 (RGFP109) is an HDAC inhibitor that can cross the brain barrier, acting on HDAC1 and HDAC3, the IC50 was 60 nM and 50 nM, respectively. RG2833 (RGFP109) is a brain-penetrating HDAC inhibitor that acts on HDAC1 and HDAC3 with an IC50 of 60 nM and 50 nM, respectively, in a cell-free assay. |
characteristics | an orally bioavailable HDAC inhibitor that can penetrate brain tissue. |
Target | Value |
HDAC3 (Cell-free assay) | 5 nM(Ki) |
HDAC1 (Cell-free assay) | 32 nM(Ki) |