RGFP966

製品コードS7229 バッチS722905

印刷

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

C₂₁H₁₉FN₄O

分子量

362.4

CAS No.

1396841-57-8

Solubility (25°C)*

体外

DMSO

85 mg/mL (234.54 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）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 10%Tween80 3 45%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.600mg/ml (9.93mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 72 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 100 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 450 μL of ddH2O to make it clear. Volume up to 1 mL. 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は、無細胞アッセイにおいてIC50が0.08 μMのHDAC3阻害剤であり、他のHDACと比較して200倍以上の選択性を示します。
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. This compound 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. It 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. This chemical causes a significant reduction in DNA replication fork velocity within the first hour of drug treatment.
in vivo	RGFP966 treatment (10 mg/kg) enhances long-term memory for object memory. This compound (3 or 10 mg/kg, s.c.) facilitates extinction and prevents reinstatement of cocaine- conditioned place preference.

プロトコル(参考用のみ)

キナーゼアッセイ	Deacetylation assays
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/23297220/
https://pubmed.ncbi.nlm.nih.gov/23894374/

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：

HSD17B4 deficiency causes dysregulation of primary cilia and is alleviated by acetyl-CoA [ Nat Commun, 2025, 16(1):2663]	PubMed: 40102401
CPSF6-RARγ interacts with histone deacetylase 3 to promote myeloid transformation in RARG-fusion acute myeloid leukemia [ Nat Commun, 2025, 16(1):616]	PubMed: 39805830
A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8]	PubMed: 40147445
Engineering a multilayered 3D stromal barrier model for quantitative analysis of T cell infiltration and cytotoxicity [ Acta Biomater, 2025, S1742-7061(25)00677-4]	PubMed: 40939760
Targeting HDAC3 Suppresses Ferroptosis and Demyelination in White Matter Injury by Restoring PDK4-Mediated Iron Homeostasis [ CNS Neurosci Ther, 2025, 31(6):e70471]	PubMed: 40485011
Regulation of FOXM1 by HDAC3 Inhibition Ameliorates Macrophage Endoplasmic Reticulum stress and Apoptosis in Mycobacterium tuberculosis Infection [ Immunobiology, 2025, 230(2):152879]	PubMed: 39938455
HDAC3 Regulates Ferroptosis via Nrf2-GPX4 Signaling in Colorectal Cancer Cells [ Dokl Biochem Biophys, 2025, 10.1134/S1607672925600496]	PubMed: 40947430
HDAC3 integrates TGF-β and microbial cues to program tuft cell biogenesis and diurnal rhythms in mucosal immune surveillance [ Sci Immunol, 2024, 9(99):eadk7387]	PubMed: 39331726
Unbiased screening identifies regulators of cell-cell adhesion and treatment options in pemphigus [ Nat Commun, 2024, 15(1):8044]	PubMed: 39271654
The lysine methyltransferase SMYD2 facilitates neointimal hyperplasia by regulating the HDAC3-SRF axis [ Acta Pharm Sin B, 2024, 14(2):712-728]	PubMed: 38322347

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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