RG2833 (RGFP109)

Catalog No.S7292 Batch:S729203

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Technical Data

Formula

C20H25N3O2
Molecular Weight 339.43 CAS No. 1215493-56-3
Solubility (25°C)* In vitro DMSO 68 mg/mL (200.33 mM)
Ethanol 13 mg/mL (38.29 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

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.
Targets
HDAC3 [1]
(Cell-free assay)		 HDAC1 [1]
(Cell-free assay)
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 LevoDOPA-induced dyskinesia. [3]
Features Orally bioavailable, HDAC inhibitor that penetrates into brain tissue.

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    KIKI mice

  • Dosages

    ~150 mg/kg

  • Administration

    Subcutaneous injection

Customer Product Validation

Data from [Data independently produced by , , Sci Rep, 2017, 7:43575]

Data from [Data independently produced by , , Neurochem Res, 2016, 41(12):3192-3205]

Data from [Data independently produced by , , The Winthrop McNair Research Bulletin, 2015, 1:17-22.]

Selleck's RG2833 (RGFP109) has been cited by 24 publications

Impact of histone deacetylase inhibition and arimoclomol on heat shock protein expression and disease biomarkers in primary culture models of familial ALS [ Cell Stress Chaperones, 2024, 29(3):359-380] PubMed: 38570009
HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364] PubMed: 38284882
Differential regulation of H3K9/H3K14 acetylation by small molecules drives neuron-fate-induction of glioma cell [ Cell Death Dis, 2023, 14(2):142] PubMed: 36805688
αKG-driven RNA polymerase II transcription of cyclin D1 licenses malic enzyme 2 to promote cell-cycle progression [ Cell Rep, 2023, 42(7):112770] PubMed: 37422761
HDAC3-Regulated PGE2 Production by Microglia Induces Phobic Anxiety Susceptibility After Stroke and Pointedly Exploiting a Signal-Targeted Gamma Visual Stimulation New Therapy [ Front Immunol, 2022, 13:845678] PubMed: 35251047
Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883] PubMed: 36230806
NADPH levels affect cellular epigenetic state by inhibiting HDAC3-Ncor complex [ Nat Metab, 2021, 3(1):75-89] PubMed: 33462516
The Effects of Selective Inhibition of Histone Deacetylase 1 and 3 in Huntington's Disease Mice [ Front Mol Neurosci, 2021, 14:616886] PubMed: 33679321
Epigenetic Heterogeneity in Friedreich Ataxia Underlies Variable FXN Reactivation [ Front Neurosci, 2021, 15:752921] PubMed: 34899161
HDAC3 inhibition ameliorates ischemia/reperfusion-induced brain injury by regulating the microglial cGAS-STING pathway [ Theranostics, 2020, 10(21):9644-9662] PubMed: 32863951

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.