RG2833(RGFP109),Brain-penetrantHDACInhibitor

How to Use:

In vitro:  RG2833 was used at 10 µM final concentration in vitro and cellular assays.

In vivo: RG2833 (RGFP109) could be dosed to KIKI mice by subcutaneous injection at 150 mg/kg, correct frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice without acute toxicity signs. RG2833 could be orally dosed to mice at 30 mg/kg, alleviate established l-DOPA-induced dyskinesia.

Reference:

• 1.      Rai M, et al. Two new pimelic diphenylamide HDAC inhibitors induce sustained frataxin upregulation in cells from Friedreich's ataxia patients and in a mouse model. (2010) PLoS One.  5(1), e8825.
• 2.      Sandi C, et al. Prolonged treatment with pimelic o-aminobenzamide HDAC inhibitors ameliorates the disease phenotype of a Friedreich ataxia mouse model. (2011) Neurobiol Dis. 42(3), 496-505.
• 3.    Johnston TH, et al. RGFP109, a histone deacetylase inhibitor attenuates L-DOPA-induced dyskinesia in the MPTP-lesioned marmoset: a proof-of-concept study. (2013) Parkinsonism Relat Disord. 19(2), 260-264.