RG2833 (RGFP109)

製品コードS7292 バッチS729201

化学情報

	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	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]
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
キナーゼアッセイ	Deacetylation assays 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

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：

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
HDAC3 inhibition ameliorates ischemia/reperfusion-induced brain injury by regulating the microglial cGAS-STING pathway [ Theranostics, 2020, 10(21):9644-9662]	PubMed: 32863951
Targeting NAD+ Biosynthesis Overcomes Panobinostat and Bortezomib-Induced Malignant Glioma Resistance [ Mol Cancer Res, 2020, 18(7):1004-1017]	PubMed: 32238439
AKT1 E17K inhibits cancer cell migration by abrogating β-catenin signaling [ Mol Cancer Res, 2020, molcanres.0623.2020]	PubMed: 33303690

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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