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Trichostatin A

Trichostatin A

产品编号 T6270   CAS 58880-19-6
别名: 曲古柳菌素A, 曲古抑菌素A, TSA

Trichostatin A (TSA) 属于二烯异羟肟酸类的天然衍生物。Trichostatin A 是一种组蛋白去乙酰化酶抑制剂 (IC50=1.8 nM),具有可逆性和特异性。Trichostatin A 导致核心组蛋白过度乙酰化,从而调节染色质结构。

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Trichostatin A Chemical Structure
Trichostatin A, CAS 58880-19-6
规格 价格/CNY 货期 数量
1 mg ¥ 568 现货
2 mg ¥ 858 现货
5 mg ¥ 1,757 现货
10 mg ¥ 2,577 现货
25 mg ¥ 3,950 现货
50 mg ¥ 5,650 现货
100 mg ¥ 8,950 现货
1 mL * 10 mM (in DMSO) ¥ 1,448 现货
产品目录号及名称: Trichostatin A (T6270)
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纯度: 98.3%
纯度: 98.05%
纯度: 97.35%
纯度: 97%
纯度: 96.32%
纯度: 96.03%
纯度: 96.01%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Trichostatin A (TSA) is a natural derivative of diene isohydroxamic acids. Trichostatin A is a histone deacetylase inhibitor (IC50=1.8 nM) that is reversible and specific. Trichostatin A leads to the hyperacetylation of core histones, which regulates chromatin structure.
靶点活性 HDAC:1.8 nM
体外活性 方法:八种乳腺癌细胞 MCF-7、T-47D、ZR-75-1、BT-474、MDA-MB-231、MDA-MB-453、CAL 51 和 SK-BR-3 用 Trichostatin A (10−12 -10−5 M) 处理 96 h,使用 SRB 方法检测细胞活力。
结果:Trichostatin A 抑制八种乳腺癌细胞系的增殖,平均 IC50=124.4±120.4 nM(范围 26.4-308.1 nM)。[1]
方法:食管鳞状细胞癌细胞 EC9706 和 EC1 用 Trichostatin A (0.3-1μM) 处理 48 h,使用 Flow Cytometry 方法检测细胞凋亡情况。
结果:在 0.3 和 0.5 μM Trichostatin A 的剂量下,早期凋亡的百分比没有显著增加。但与对照组相比,1.0 μM Trichostatin A 处理可显著诱导早期细胞凋亡。此外,中晚期凋亡的百分比以浓度依赖的方式增加。[2]
方法:食管鳞状细胞癌细胞 EC9706 和 EC1 用 Trichostatin A (0.3-1μM) 处理 60 min,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Trichostatin A 以剂量依赖的方式降低 PI3K 的蛋白水平以及 p-Akt 和 p-ERK1/2。组蛋白H4的乙酰化以浓度依赖性方式增加。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Trichostatin A (500 μg/kg) 皮下注射给 NMU 诱导乳腺癌肿瘤的大鼠,每天一次,持续四周。
结果:Trichostatin A 在体内具有显著的抗肿瘤活性。Trichostatin A 处理的大鼠肿瘤具有良性表型,纤维腺瘤或管状腺瘤,这表明 Trichostatin A 的抗肿瘤活性可能归因于分化的诱导。[1]
方法:为检测体内抗肿瘤活性,将 Trichostatin A (0.5-1 mg/kg,每周两次) 和 Quercetin (10 mg/kg,每周三次) 腹腔注射给携带人肺腺癌肿瘤 A549 的裸鼠,持续十三周。
结果:高剂量 Trichostatin A 显著抑制肿瘤生长,而低剂量 Trichostatin A 和 Quercetin 单独使用没有效果。然而,低剂量 Trichostatin A 和 Quercetin 联合治疗显著抑制了肿瘤生长。[3]
激酶实验 In vitro HDAC activity: Total cellular extracts are prepared from each breast cancer cell line (MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, or SK-BR-3). A 20 μL crude cell extract (~2.5 ×105 cells), in the presence of varying concentrations of Trichostatin A in 0.1% (v/v) ethanol or 0.1% (v/v) ethanol as vehicle control, are incubated for 60 minutes at 25 °C with 1 μL (~1.5 × 106 cpm) of [3H]acetyl-labeled histone H4 peptide substrate (NH2-terminal residues 2-20) that has been acetylated with [3H]acetic acid, sodium salt (3.7 GBq/mmol) by an in vitro incorporation method. Each 200 μL reaction is quenched with 50 μL of 1 M HCl/0.16 M acetic acid and extracted with 600 μL of ethyl acetate, and released [3H]acetate is quantified by scintillation counting. IC50 values are determined graphically using nonlinear regression to fit inhibition data to the appropriate dose-response curve.
细胞实验 Cells are exposed to various concentrations of Trichostatin A for 96 hours. After treatment, cell proliferation is estimated using the sulforhodamine B colorimetric assay. Cell viability is determined by trypan blue exclusion. (Only for Reference)
别名 曲古柳菌素A, 曲古抑菌素A, TSA
化合物与蛋白结合的复合物

T6270_2

CRYSTAL STRUCTURE OF AN HDAC HOMOLOG COMPLEXED WITH TRICHOSTATIN A

分子量 302.37
分子式 C17H22N2O3
CAS No. 58880-19-6

存储

store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 15.1 mg/mL (50 mM)

Ethanol: 3 mg/mL (10 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 3.3072 mL 16.536 mL 33.0721 mL 82.6802 mL
5 mM 0.6614 mL 3.3072 mL 6.6144 mL 16.536 mL
10 mM 0.3307 mL 1.6536 mL 3.3072 mL 8.268 mL
DMSO 20 mM 0.1654 mL 0.8268 mL 1.6536 mL 4.134 mL
50 mM 0.0661 mL 0.3307 mL 0.6614 mL 1.6536 mL

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参考文献

1. Vigushin DM, et al. Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo. Clin Cancer Res. 2001 Apr;7(4):971-6. 2. Ma J, et al. Trichostatin A, a histone deacetylase inhibitor, suppresses proliferation and promotes apoptosis of esophageal squamous cell lines. Mol Med Rep. 2015 Jun;11(6):4525-31. 3. Chan ST, et al. Quercetin enhances the antitumor activity of trichostatin A through upregulation of p53 protein expression in vitro and in vivo. PLoS One. 2013;8(1):e54255. 4. Huang W, et al. J Biol Chem, 2005, 280(11), 120047-120054. 5. Avila AM, et al. J Clin Invest, 2007, 117(3), 659-671. 6. Li X, Pan L, Wang B, et al. The Histone Deacetylases HosA and HdaA Affect the Phenotype and Transcriptomic and Metabolic Profiles of Aspergillus niger[J]. Toxins. 2019, 11(9): 520. 7. Meng Y, Qian X, Zhao L, et al. Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma[J]. Cancer Cell International. 2021, 21(1): 1-12. 8. Xu K, Sun G, Li M, et al. Glibenclamide Targets Sulfonylurea Receptor 1 to Inhibit p70S6K Activity and Upregulate KLF4 Expression to Suppress Non-Small Cell Lung Carcinoma[J]. Molecular cancer therapeutics. 2019, 18(11): 2085-2096. 9. Su Q, Li T, He P F, et al. Trichostatin A ameliorates Alzheimer’s disease-related pathology and cognitive deficits by increasing albumin expression and Aβ clearance in APP/PS1 mice[J]. Alzheimer's Research & Therapy. 2021, 13(1): 1-15.

文献引用

1. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22. 2. Liang X L, Ouyang L, Yu N N, et al.Histone deacetylase inhibitor pracinostat suppresses colorectal cancer by inducing CDK5-Drp1 signaling-mediated peripheral mitofission.Journal of Pharmaceutical Analysis.2023 3. Guo Q, Jing Y, Gao Y, et al.The PIF1/PIF3‐MED25‐HDA19 transcriptional repression complex regulates phytochrome signaling in Arabidopsis.New Phytologist.2023 4. Su Q, Li T, He P F, et al. Trichostatin A ameliorates Alzheimer’s disease-related pathology and cognitive deficits by increasing albumin expression and Aβ clearance in APP/PS1 mice. Alzheimer's Research & Therapy. 2021 Jan 4;13(1):7. doi: 10.1186/s13195-020-00746-8. 5. Yuting Meng,Xixi Qian,Li Zhao,Nan Li,Shengjie Wu,Baoan Chen,Tong Sun,Xuerong Wang Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma. Cancer Cell International. 2021, 21(1): 1-12. 6. Zhang L, Shi J, Du D, et al. Ketogenesis acts as an endogenous protective programme to restrain inflammatory macrophage activation during acute pancreatitis. eBioMedicine. 2022, 78: 103959. 7. Li X, Pan L, Wang B, et al. The Histone Deacetylases HosA and HdaA Affect the Phenotype and Transcriptomic and Metabolic Profiles of Aspergillus niger. Toxins. 2019, 11(9): 520. 8. Xu K, Sun G, Li M, et al. Glibenclamide Targets Sulfonylurea Receptor 1 to Inhibit p70S6K Activity and Upregulate KLF4 Expression to Suppress Non-Small Cell Lung Carcinoma. Molecular cancer therapeutics. 2019, 18(11): 2085-2096. 9. Du T, Hu X, Hou Z, et al.Re-expression of epigenetically silenced PTPRR by histone acetylation sensitizes RAS-mutant lung adenocarcinoma to SHP2 inhibition.Cellular and Molecular Life Sciences.2024, 81(1): 1-14.
HDAC-IN-52 AR42 KH16 SR-4370 BChE/HDAC6-IN-1 Oxamflatin Valproic Acid HDAC6-IN-19

相关化合物库

该产品包含在如下化合物库中:
微生物天然产物库 抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 已知活性化合物库 高通量筛选天然产物库 表观遗传库 抗癌化合物库 Ro5类药天然产物库 临床期小分子药物库

剂量换算

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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
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Keywords

Trichostatin A 58880-19-6 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases inhibit Inhibitor 曲古柳菌素A 曲古抑菌素A TSA inhibitor

 

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