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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。
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。
规格 | 价格 | 库存 | 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 x 10 mM (in DMSO) | ¥ 1,448 | 现货 |
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 | 曲古抑菌素A, 曲古柳菌素A, TSA |
分子量 | 302.37 |
分子式 | C17H22N2O3 |
CAS No. | 58880-19-6 |
Smiles | C[C@H](\C=C(/C)\C=C\C(=O)NO)C(=O)c1ccc(cc1)N(C)C |
密度 | 1.139 g/cm3 |
存储 | store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (165.36 mM), Sonication is recommended. Ethanol: 3 mg/mL (10 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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