RG2833 (RGFP109) --- Brain-penetrant HDAC Inhibitor

RG2833 (RGFP109) is a potent and selective brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. It upregulates frataxin mRNA and protein levels dose-dependently in cultures of unstimulated peripheral blood mononuclear cells (PBMC) obtained from FRDA patients. In vivo it corrects frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice without acute toxicity signs.

Product information

CAS Number: 1215493-56-3

Molecular Weight: 339.43

Formula: C20H25N3O2

Chemical Name: N-(6-((2-aminophenyl)amino)-6-oxohexyl)-4-methylbenzamide

Smiles: CC1C=CC(=CC=1)C(=O)NCCCCCC(=O)NC1=CC=CC=C1N

InChiKey: VOPDXHFYDJAYNS-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

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.

References:

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.

Products are for research use only. Not for human use.

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