RGFP966

製品コード：S7229 純度：99.74%

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.

CAS No. 1396841-57-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 74500	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（111）

製品安全説明書

現在のバッチを見る：純度： 99.74%

99.74

RGFP966と併用されることが多い化合物

Tubastatin A

RGFP966 and Tubastatin A decrease total HDAC activity in HLMVEC and reduce the inflammatory and hyper-permeability response to LPS in mice.

Birmpas C, et al. The FASEB Journal 29 (2015): 411-4.

(+)-JQ1

RGFP966 and JQ1 dramatically reduces tumor volume and growth rate and suppresses tumor growth via induction of apoptosis in the glioma xenograft mouse model.

Wang Q, et al. Mol Cancer Ther. 2020 Dec;19(12):2542-2553.

TSA (Trichostatin A)

RGFP966 and Trichostatin A increases the expression of AKAP12 at both the mRNA and protein levels.

He P, et al. Int J Oncol. 2018 Apr;52(4):1305-1316.

RGFP966関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
関連製品	Entinostat (MS-275) TSA (Trichostatin A) Mocetinostat (MGCD0103) Tubastatin A Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) 2HCl MC1568 Tubastatin A HCl PCI-34051 Tacedinaline (CI994) LMK-235 Fimepinostat (CUDC-907) Tubacin Givinostat (ITF2357) TMP269 AR-42 Sodium butyrate Pracinostat (SB939) Santacruzamate A (CAY10683) Abexinostat (PCI-24781) (-)-Parthenolide CUDC-101 Dacinostat (LAQ824) CAY10603 RG2833 (RGFP109) Tasquinimod Tucidinostat (Chidamide) TMP195 Nexturastat A Droxinostat Domatinostat (4SC-202) Scriptaid 4-PBA (4-Phenylbutyric acid) M344 Resminostat Citarinostat (ACY-241) BG45 WT161 ACY-738 HPOB ITSA-1 (ITSA1) Tubastatin A TFA TC-H 106 SIS17 ACY-775 BML-210 (CAY10433) TH34 Raddeanin A	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HH and Hut78 cells	Proliferation assay	10 μM	0, 24, 48, 72 h	Both cell lines were sensitive to treatment with 10 μM 966. However, Hut78 cells exhibited a greater sensitivity than HH cells.	23894374
Em-Myc lymphoma cells	Function assay	≤1 μM	48 h	Cell proliferated significantly more slowly than vehicle-treated controls in the presence or absence of pro-survival BCL-2 overexpression	26447190
APL cells	Function assay	≤2 μM	48 h	RGFP966 did not induce apoptosis in APL cells but did reduce clonogenicity and increased maturation.	26447190
HH	Function assay	10 μM	24 h	increases the acetylation at H3K9/K14, H3K27, and H4K5	23894374
Hut78	Function assay	10 μM	24 h	increases the acetylation at H3K9/K14, H3K27, and H4K5	23894374
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM.	29940115
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM.	29940115
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM.	29940115
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM.	29940115
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM.	29940115
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM.	29940115
Sf9	Function assay		60 mins	Inhibition of full length human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 insect cells using substrate measured after 60 mins by colorimetric method	29541372
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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.

Targets

HDAC3 ^[1]
(Cell-free assay)

80 nM

In Vitro
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]
Kinase Assay	Deacetylation assays
Kinase Assay	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.
細胞実験	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.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	p-STAT3 / Acetyl-STAT3 / STAT3 / Ac-H3 / Ac-H4 H3K9K14ac / H3 / H3K56ac / H3K27ac / H4K5ac		28338101

In Vivo
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]
動物実験	動物モデル	Mouse
	投与量	10 mg/kg, 10.0 mL/kg
	投与経路	s.c.

参考
[1] Malvaez M, et al. PNAS, 2013, 110(7), 2647-2652. [2] Wells CE, et al. PLoS One, 2013, 8(7), e68915.

参考

化学情報

分子量	362.4	化学式	C₂₁H₁₉FN₄O
CAS No.	1396841-57-8	SDF	Download RGFP966 SDFをダウンロードする
Smiles	C1=CC=C(C=C1)C=CCN2C=C(C=N2)C=CC(=O)NC3=C(C=C(C=C3)F)N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 72 mg/mL ( (198.67 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	5.0mg/ml (13.80mM)	Taking the 1 mL working solution as an example, add 100 μL of 50 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 450 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 Corn oil	3.6mg/ml (9.93mM)	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.
Clear solution	5%DMSO 1 40%PEG300 2 10%Tween80 3 45%ddH2O	3.6mg/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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問1:
Does this product S7229 specifically inhibit HDAC3? Or does it target other HDACs as well?

回答
In the paper, it is indicated that "RGFP966 is specific for HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM. ". However, we did not preform experiment to confirm this data. Please refer to the following link for detailed information: http://www.pnas.org/content/110/7/2647.long

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