TSA (Trichostatin A)

製品コードS1045 バッチS104513

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H22N2O3
分子量 302.4 CAS No. 58880-19-6
Solubility (25°C)* 体外 DMSO 60 mg/mL (198.41 mM)
Water Insoluble
 
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
2%DMSO 30%PEG300 2%Tween80 66%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.500mg/ml (4.96mM) Taking the 1 mL working solution as an example, add 20 μL of 75 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 トリコスタチンA (TSA (Trichostatin A) ) は HDAC 阻害剤であり、IC50 は cell-free assay において < 1.8 nM です。
in vitro TSA (Trichostatin A) inhibits the proliferation of eight breast carcinoma cell lines including MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3 with mean IC50 of 124.4 nM (range, 26.4-308.1 nM), with more potency against cell lines that express ERα than the ERα-negative cell lines. It inhibits HDAC activity similarly in all the breast cancer cell lines with mean IC50 of 2.4 nM (range, 0.6-2.6 nM), and results in pronounced histone H4 hyperacetylation. [1] Unlike Trapoxin (TPX) and Chlamydocin which potently inhibit HDAC1 or HDAC4 but not HDAC6, this compound inhibits these HDACs to a similar extent with IC50 of 6 nM, 38 nM, and 8.6 nM, respectively. [2] Treatment with it (100 ng/mL) induces the expression of transforming growth factor β type II receptor (TβRII) in MIA PaCa-2 cells through the recruitment of p300 and PCAF into a Sp1-NF-Y HDAC complex that binds the DNA element of TβRII promoter, which is associated with a concomitant acetylation of Sp1 and an overall decrease in the amount of HDAC associated with the complex. [4]
in vivo Administration of TSA (Trichostatin A) at 0.5 mg/kg for 4 weeks displays potent antitumor activity in the N-methyl-N-nitrosourea carcinogen-induced rat mammary carcinoma model, without any measurable toxicity at doses up to 5 mg/kg. [1] Single intraperitoneal doses of 10 mg/kg of this compound in nontransgenic and spinal muscular atrophy (SMA) model mice results in increased levels of acetylated H3 and H4 histones and modest increases in survival motor neuron (SMN) gene expression. Its administration at 10 mg/kg/day improves survival, attenuates weight loss, and enhances motor behavior in the SMA model mice. [5]

プロトコル(参考用のみ)

キナーゼアッセイ 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 TSA (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.
細胞アッセイ 細胞株 MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3
濃度 Dissolved in absolute ethanol, final concentrations ~10 μM
反応時間 96 hours
実験の流れ

Cells are exposed to various concentrations of TSA (Trichostatin A) for 96 hours. After treatment with this compound, cell proliferation is estimated using the sulforhodamine B colorimetric assay. Cell viability is determined by trypan blue exclusion.
動物実験 動物モデル Inbred virgin female (Ludwig/Wistar/Olac) rats bearing tumors induced with NMU
投薬量 ~5 mg/kg/day
投与方法 Injection s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/11309348/
  • https://pubmed.ncbi.nlm.nih.gov/11134513/
  • https://pubmed.ncbi.nlm.nih.gov/14612526/
  • https://pubmed.ncbi.nlm.nih.gov/15647279/
  • https://pubmed.ncbi.nlm.nih.gov/17318264/

カスタマーフィードバック

Data from [Biochem Biophys Res Commun, 2014, 10.1016/j.bbrc.2014.01.184]

Data from [Biochem Biophys Res Commun, 2014, 10.1016/j.bbrc.2014.01.184]

Data from [Epigenetics, 2012, 7(10):1161-72]

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人間や獣医の診断であるか治療的な使用のためにでない。

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