TSA (Trichostatin A)

製品コードS1045 バッチS104506

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
Ethanol Insoluble
* <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 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. Trichostatin A 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, Trichostatin A inhibits these HDACs to a similar extent with IC50 of 6 nM, 38 nM, and 8.6 nM, respectively. [2] Trichostatin A (100 ng/mL) treatment 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 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 Trichostatin A 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. Administration of Trichostatin A 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 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 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.
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.

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Glucocorticoids increase adiposity by stimulating Krüppel-like factor 9 expression in macrophages [ Nat Commun, 2024, 15(1):1190] PubMed: 38331933
Acetylation-dependent regulation of core spliceosome modulates hepatocellular carcinoma cassette exons and sensitivity to PARP inhibitors [ Nat Commun, 2024, 15(1):5209] PubMed: 38890388
Replication fork stalling in late S-phase elicits nascent strand degradation by DNA mismatch repair [ Nucleic Acids Res, 2024, gkae721] PubMed: 39180395
Unveiling the mechanism of broad-spectrum blast resistance in rice: The collaborative role of transcription factor OsGRAS30 and histone deacetylase OsHDAC1 [ Plant Biotechnol J, 2024, 10.1111/pbi.14299] PubMed: 38294722
Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5] PubMed: 38823394
Sirt5 improves cardiomyocytes fatty acid metabolism and ameliorates cardiac lipotoxicity in diabetic cardiomyopathy via CPT2 de-succinylation [ Redox Biol, 2024, 73:103184] PubMed: 38718533
Targeting histone deacetylase 6 (HDAC6) to enhance radiation therapy in meningiomas in a 2D and 3D in vitro study [ EBioMedicine, 2024, 105:105211] PubMed: 38917510
PTPLAD1 Regulates PHB-Raf Interaction to Orchestrate Epithelial-Mesenchymal and Mitofusion-Fission Transitions in Colorectal Cancer [ Int J Biol Sci, 2024, 20(6):2202-2218] PubMed: 38617530
The ARID1A-METTL3-m6A axis ensures effective RNase H1-mediated resolution of R-loops and genome stability [ Cell Rep, 2024, 43(2):113779] PubMed: 38358891
GCN5 mediates DNA-PKcs crotonylation for DNA double-strand break repair and determining cancer radiosensitivity [ Br J Cancer, 2024, 10.1038/s41416-024-02636-4] PubMed: 38575732

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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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