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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H19FN4O |
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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 | |||
* <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. |
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. |
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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] |
キナーゼアッセイ | Deacetylation assays | |
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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. |
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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]
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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