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RGFP966

RGFP966

产品编号 T1762   CAS 1357389-11-7
别名: RGFP 966

RGFP966 是一种能够透过血脑屏障的高选择性HDAC3抑制剂,IC50为 80 nM。

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RGFP966 Chemical Structure
RGFP966, CAS 1357389-11-7
规格 价格/CNY 货期 数量
1 mg ¥ 315 现货
2 mg ¥ 453 现货
5 mg ¥ 738 现货
10 mg ¥ 946 现货
25 mg ¥ 1,930 现货
50 mg ¥ 3,490 现货
100 mg ¥ 4,970 现货
1 mL * 10 mM (in DMSO) ¥ 815 现货
其他形式的 RGFP966:
产品目录号及名称: RGFP966 (T1762)
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选择批次  
纯度: 99.77%
纯度: 99.44%
纯度: 99.2%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 RGFP966 is an HDAC3 inhibitor (IC50: 0.08 μM) and does not affect other HDACs at concentrations up to 15 μM.
靶点活性 HDAC3:80 nM(cell free)
体外活性 RGFP966 is specific for HDAC3 (IC50: 0.08 μM) and no effective inhibition of any other HDAC at concentrations up to 15 μM [1]. In LPS/IFNγ-stimulated RAW 264.7 macrophages treatment with RGFP966 did not change the expression of the genes TNFα, iNOS, and IL-10 but provided a significant downregulation of the expression of the pro-inflammatory genes IL-1β, IL-6 and IL-12b [2]. RGFP966 resulted in decreased cell growth in CTCL cell lines due to increased apoptosis that was associated with DNA damage and impaired S phase progression [3].
体内活性 All mice exhibited a robust preference for the cocaine-paired context after cocaine-conditioned place preference (CPP) training. Treatment with RGFP966 (3 or 10 mg/kg, s.c.)immediately after the drug-free preference tests resulted in significant extinction of CPP on posttest 2 and posttest 3. Treatment with 10 mg/kg, but not with 3 mg/kg, resulted in a significantly rapid reduction of CPP on the subsequent days [1]. RGFP966 at doses of 10 and 25 mg/kg improves motor deficits on rotarod and in open field exploration, accompanied by neuroprotective effects on striatal volume [4].
激酶实验 Briefly, the respective human recombinant HDAC enzymes were incubated in the absence and/or in presence of various concentrations RGFP966 and a pro-fluorogenic substrate at room temperature for 60 min. Next, the deacetylation reaction was stopped by the addition of the HDAC Stop Solution (6 mg/ml trypsin, 0.3 mM SAHA) in all wells and the plate was incubated at 37 °C for 20 min. The release of the fluorescent 7-amino-4-methylcoumarin was monitored by measuring the fluorescence at λem = 460 nm and λex = 390 nm using a Synergy H1 plate reader. The fluorescence value of the background wells was subtracted from the fluorescence of the positive control, blank and inhibitor wells. Nonlinear regression was used to fit the data to the log(inhibitor) vs. response curve using GraphPad Prism [2].
细胞实验 To investigate the influence of the HDAC 3-selective inhibitor RGFP966 on cell viability, RAW 264.7 macrophages, HBE cells and hASM cells were seeded in 96-well plates. To obtain identical cell density at the start of the experiments, RAW 264.7 macrophages were seeded at 25,000 cells/cm2, HBE cells and hASM cells were seeded at 70% confluency (based on surface area) and were serum-starved for 24 h prior incubation with RGFP966. Shortly before incubation with RGFP966, the medium was replaced by 100 μl fresh (if appropriate serum free) culture medium. Incubations with LPS and IFNγ were performed as described for HDAC 1–3 downregulation by siRNA. After 20 h of incubation with RGFP966, 20 μl of CellTiter 96 AQueous One Solution reagent was added to each well and incubated at 37 °C for 1 h in the dark. The absorbance at 490 nm was measured using a Synergy H1 plate reader. LPS/IFNγ-stimulated cells without addition of RGFP966 were considered 100% [2].
动物实验 Subthreshold training and a 24-h retention test for location-dependent object recognition memory (OLM) and novel object recognition memory (ORM) were performed as described previously. Mice received an injection of RGFP966 (3, 10, or 30 mg/kg s.c) or vehicle alone either 1 h before or immediately after a 3-min training seeion [1].
别名 RGFP 966
分子量 362.4
分子式 C21H19FN4O
CAS No. 1357389-11-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 360 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Malvaez M, et al. HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52. 2. Leus NG, et al. HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity. Biochem Pharmacol. 2016 May 15;108:58-74. 3. Wells CE, et al. Inhibition of histone deacetylase 3 causes replication stress in cutaneous T cell lymphoma. PLoS One. 2013 Jul 22;8(7):e68915. 4. Jia H, et al. The Effects of Pharmacological Inhibition of Histone Deacetylase 3 (HDAC3) in Huntington's Disease Mice. PLoS One. 2016 Mar 31;11(3):e0152498.
BRD2492 ACY-738 LMK-235 Crebinostat 1-Naphthohydroxamic acid RG2833 Fimepinostat Rac-Belinostat

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 含氟化合物库 组蛋白修饰化合物库 已知活性化合物库 抗癌化合物库 抗胰腺癌化合物库 DNA 损伤和修复分子库 NO PAINS 化合物库 抗乳腺癌化合物库 NF-κB 通路分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

RGFP966 1357389-11-7 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC inhibit Histone deacetylases Inhibitor RGFP 966 RGFP-966 inhibitor

 

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