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HSF1A

HSF1A

产品编号 T4125   CAS 1196723-93-9

HSF1A 是一种可渗透细胞的 HSF1 激活剂,可保护哺乳动物细胞免受应激诱导的细胞凋亡。它还是 TRiC/CCT 的特异性抑制剂。

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HSF1A Chemical Structure
HSF1A, CAS 1196723-93-9
规格 价格/CNY 货期 数量
1 mg ¥ 549 现货
2 mg ¥ 798 现货
5 mg ¥ 1,220 现货
10 mg ¥ 1,800 现货
25 mg ¥ 3,970 现货
50 mg ¥ 5,680 现货
100 mg ¥ 7,930 现货
1 mL * 10 mM (in DMSO) ¥ 1,120 现货
产品目录号及名称: HSF1A (T4125)
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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 HSF1A is a cell-permeable activator of HSF1 that protects mammalian cells against stress-induced apoptosis.
体外活性 HSF1A is a small-molecule activator of HSF1 that protects cells from stress-induced apoptosis, binds TRiC subunits and inhibits TRiC activity without perturbation of ATP hydrolysis. Genetic inactivation or depletion of the TRiC complex results in human HSF1 activation and HSF1A inhibits the direct interaction between purified TRiC and HSF1 in vitro. Moreover, fluorescence anisotropy experiments using FITC coupled to HSF1A demonstrates that HSF1A-FITC binds to a purified Tcp1 subunit of TRiC with an affinity of approximately 600 nM. This is validated qualitatively via titration of purified Tcp1 into binding reactions containing 500 nM Biotin or HSF1A-Biotin. Quantification by counting the number of cell containing aggregates as a function of the total number of cells reveals that at HSF1A concentrations as low as 2 μM, a reduced number of aggregate-containing cells are observed. The fraction of cells containing aggregates continued to decrease in a dose-dependent manner such that pretreatment with 12 μM HSF1A resulta in ~20% of the cells exhibiting aggregates visible by fluorescence microscopy.
体内活性 HSF1A enhances HSF1 activity, stabilizes HSF1 expression and minimizes Doxorubicin (DOX)-induced cardiac damage. WKY rats are challenged with DOX (accumulated dose: 30 mg/kgw), and DOX combined with HSF1A (100 mg/kgw/day). Supplementation with HSF1A significantly elevates cardiac functions back to the levels of the control group. HSF1A has been shown to stimulate human HSF1 nuclear translocation, elevate protein chaperone expression and ameliorate protein misfolding and cell death in a neurodegenerative disease model. The echocardiographic results exhibit that HSF1A also alleviates DOX-induced failures in cardiac function as well.
激酶实验 Protein extracts are generated from mammalian, yeast and E. coli cultures using biotin-binding buffer (20 mM HEPES, 5 mM MgCl2, 1 mM EDTA, 100 mM KCl, 0.03% NP-40) supplemented with 1% Trition-X100 and protease inhibitors. Approximately 0.5 mg of protein extract is incubated with 100 μM HSF1A-Biotin for 4 h at 4°C and HSF1A-Biotin associated proteins captured by with NeutrAvidin Agarose Resin. After washing in biotin binding buffer proteins are eluted using 50 μL biotin elution buffer (100 mM Tris, 150 mM NaCl, 0.1 mM EDTA, 2 mM D-biotin), resolved on a 4-20% SDS-PAGE, and immunoblotted. For purified TRiC and Hsp70 analyses, 5 nM protein is incubated in biotin-binding buffer+0.5% Triton X-100 with 100 μM biotin or 100 μM HSF1A-Biotin for 4 h at 4°C and captured with NeutrAvidin Resin. For NiNTA purified yeast Tcp1, different concentrations of Tcp1 0.5 μM, 1 mM, 2 mM, 3 mM and 4 mM in 25 mM Hepes pH 7.5, 150 mM NaCl are incubated with 0.5 μM Biotin or HSF1A-Biotin for 4 h at 4°C and captured with NeutrAvidin Resin.
细胞实验 PC12 cells seeded into a 96-well plate (5×104 cells/well) are treated with increasing concentrations of HSF1A (2, 4, 8 and 12 μM) for 15 h, at which time httQ74-GFP expression is stimulated by incubation in the presence of 1 μg/mL Doxycycline for 5 d. Cell viability is assessed via the XTT viability assay.
动物实验 RatTen-week-old Wistar Kyoto rats (WKY) are used. The rats are housed at a constant temperature (22°C) on a 12-h light/dark cycle with food and tap water. The animals are arranged into three groups: WKY rats (the control group), DOX rats and DOX rats treated with HSF1A. Each group contain five animals. The DOX group is injected with DOX (5?mg/kg) for 6 consecutive weeks intraperitoneal injection to achieve a cumulative dose of 30?mg/kg, which has been well documented to achieve cardiotoxicity. The small molecular HSF1 activator HSF1A (100?mg/kg/day) is injected intraperitoneally.
分子量 409.52
分子式 C21H19N3O2S2
CAS No. 1196723-93-9

存储

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

溶解度

DMSO: 150 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. Neef DW, et al. A direct regulatory interaction between chaperonin TRiC and stress-responsive transcription factor HSF1. Cell Rep. 2014 Nov 6;9(3):955-66. 2. Neef DW, et al. Modulation of heat shock transcription factor 1 as a therapeutic target for small molecule intervention in neurodegenerative disease. PLoS Biol. 2010 Jan 19;8(1):e120200291. 3. Huang CY, et al. Doxorubicin attenuates CHIP-guarded HSF1 nuclear translocation and protein stability to trigger IGF-IIR-dependent cardiomyocyte death. Cell Death Dis. 2016 Nov 3;7(11):e2455.
Tanespimycin SNX2112 AMP-PCP ML346 TRC051384 2',4'-DIHYDROXYCHALCONE HM03 TRC051384 HCl

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 转录因子库 抗乳腺癌化合物库 NO PAINS 化合物库 抗癌化合物库 经典已知活性库 细胞凋亡化合物库 已知活性化合物库 抗衰老化合物库 细胞骨架化合物库

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。
% DMSO
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% Tween 80
% 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

HSF1A 1196723-93-9 Cytoskeletal Signaling Metabolism HSP Inhibitor inhibit Heat shock proteins HSF-1A inhibitor

 

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