RG2833 (RGFP109)

製品コードS7292 バッチS729201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H25N3O2
分子量 339.43 CAS No. 1215493-56-3
Solubility (25°C)* 体外 DMSO 68 mg/mL (200.33 mM)
Ethanol 11 mg/mL (32.4 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
in vitro

RG2833 (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 (RGFP109) (150 mg/kg) corrects frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice without acute toxicity signs. [1] It ameliorates the disease phenotype of a Friedreich ataxia mouse model. [2] This compound (30 mg/kg p.o.) also alleviates established LevoDOPA-induced dyskinesia. [3]
特徴 Orally bioavailable, HDAC inhibitor that penetrates into brain tissue.

プロトコル(参考用のみ)

キナーゼアッセイ Time dependent IC50 value with pre-incubation
Deacetylation assays for RG2833 (RGFP109) are based on the homogenous fluorescence release assay. In brief, purified recombinant enzymes are incubated with serial-diluted inhibitors at various concentrations, with pre-incubation times ranging from 0 to 3 hours, in the standard HDAC buffer. Acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both HDAC1 and HDAC3) is added after the pre-incubation period. The reaction is allowed to run for 1 hour. The trypsin peptidase developer, at final concentration of 5mg/ml, is added after 1 hour, and the fluorescence emission is then measured using a Tecan M200 96-well plate reader.
動物実験 動物モデル KIKI mice
投薬量 ~150 mg/kg
投与方法 Subcutaneous injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/20098685/
  • https://pubmed.ncbi.nlm.nih.gov/21397024/
  • https://pubmed.ncbi.nlm.nih.gov/22901956/

カスタマーフィードバック

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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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