RGFP966

製品コードS7229 バッチS722904

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

C21H19FN4O
分子量 362.4 CAS No. 1396841-57-8
Solubility (25°C)* 体外 DMSO 72 mg/mL (198.67 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
3.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
in vitro RGFP966 is a slow-on/slow-off, competitive tight-binding HDAC inhibitor, with an IC50 of 0.08μM for HDAC3 and no effective inhibition of any other HDAC at concentrations up to 15μM. [1] RGFP966 treatment on two CTCL cell lines for 24 hours prior to western blot analysis resulted in increased acetylation at H3K9/K14, H3K27, and H4K5, but not H3K56ac. RGFP966 decreases cell growth in CTCL (cutaneous T cell lymphoma) cell lines due to increased apoptosis that is associated with DNA damage and impaired S phase progression. RGFP966 causes a significant reduction in DNA replication fork velocity within the first hour of drug treatment. [2]
in vivo RGFP966 treatment (10 mg/kg) enhances long-term memory for object memory. RGFP966 (3 or 10 mg/kg, s.c.) facilitates extinction and prevents reinstatement of cocaine- conditioned place preference. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Deacetylation assays
Deacetylation assays are based on the homogenous fluorescence release assay. Purified recombinant enzymes are incubated with serial-diluted inhibitors at the concentrations indicated in the figures, 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.
細胞アッセイ 細胞株 HH and Hut78 CTCL cell lines
濃度 ~10μM
反応時間 24 to 72 h
実験の流れ Cells are counted and split into T25 (Corning) flasks at 26105 cells/mL. Cells are then treated with DMSO, or HDIs once at hour 0. 100 ml aliquots are taken in triplicate from each flask at 0 hr, 24 hrs, 48 hrs, and 72 hrs after treatment, distributed into a flat bottom 96-well plate, and 10 ml of alamar blue added to each well. After a 4 hr incubation, fluorescence is measured using the Biotek Synergy MX Microplate Reader.
動物実験 動物モデル Mouse
投薬量 10 mg/kg, 10.0 mL/kg
投与方法 s.c.

カスタマーフィードバック

Data from [Data independently produced by , , Leukemia, 2017, 31(12):2761-2770]

Data from [Data independently produced by , , J Invest Dermatol, 2017, 137(9):1935-1944]

Data from [Data independently produced by , , Front Mol Neurosci, 2016, 9:131]

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：

Extracellular CIRP induces abnormal activation of fibroblast-like synoviocytes from patients with RA via the TLR4-mediated HDAC3 pathways [ Int Immunopharmacol, 2024, 128:111525] PubMed: 38218010
LncRNA CHROMR/miR-27b-3p/MET axis promotes the proliferation, invasion, and contributes to rituximab resistance in diffuse large B-cell lymphoma [ J Biol Chem, 2024, 300(3):105762] PubMed: 38367665
macroH2A2 antagonizes epigenetic programs of stemness in glioblastoma [ Nat Commun, 2023, 14(1):3062] PubMed: 37244935
The NCOR-HDAC3 co-repressive complex modulates the leukemogenic potential of the transcription factor ERG [ Nat Commun, 2023, 14(1):5871] PubMed: 37735473
The NCOR-HDAC3 co-repressive complex modulates the leukemogenic potential of the transcription factor ERG [ Nat Commun, 2023, 14(1):5871] PubMed: 37735473
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051] PubMed: 37598220
Low-dose IL-2 enhances the generation of IL-10-producing immunoregulatory B cells [ Nat Commun, 2023, 14(1):2071] PubMed: 37045832
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051] PubMed: 37598220
RANK ligand converts the NCoR/HDAC3 co-repressor to a PGC1β- and RNA-dependent co-activator of osteoclast gene expression [ Mol Cell, 2023, 83(19):3421-3437.e11] PubMed: 37751740
HDAC3 aberration-incurred GPX4 suppression drives renal ferroptosis and AKI-CKD progression [ Redox Biol, 2023, 10.1016/j.redox.2023.102939] PubMed: 37890360

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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