RG2833

• CAT Number: I000811
• CAS Number: 1215493-56-3
• Molecular Formula: C20H25N3O2
• Molecular Weight: 339.4
• Purity: ≥95%
• Synonyms: N-[6-(2-aminoanilino)-6-oxohexyl]-4-methylbenzamide
• Target: HDAC
• Solubility: DMSO 68 mg/ml; Water <1 mg/ml
• Storage: Store at -20°C
• IC50: 60 nM (HDAC1); 50 nM (HDAC3) [1]
• InChI: InChI=1S/C20H25N3O2/c1-15-10-12-16(13-11-15)20(25)22-14-6-2-3-9-19(24)23-18-8-5-4-7-17(18)21/h4-5,7-8,10-13H,2-3,6,9,14,21H2,1H3,(H,22,25)(H,23,24)
• InChIKey: VOPDXHFYDJAYNS-UHFFFAOYSA-N
• SMILES: CC1=CC=C(C=C1)C(=O)NCCCCCC(=O)NC2=CC=CC=C2N

RG2833 (Cat No.:I000811) is a brain-barrier-permeable HDAC inhibitor for HDAC1 and HDAC3 with IC50 of 60 nM and 50 nM, respectively. In unstimulated peripheral blood mononuclear cell (PBMC) culture medium, RG2833 dose-dependently up-regulates frataxin mRNA and protein levels.

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. PLoS One. 2010, 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. Neurobiol Dis. 2011, 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. Parkinsonism Relat Disord. 2013, 19(2), 260-264.