TSA (Trichostatin A)

Catalog No.S1045 Batch:S104510

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Technical Data

Formula

C17H22N2O3
Molecular Weight 302.4 CAS No. 58880-19-6
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description TSA (Trichostatin A) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Targets
HDAC [1]
(Cell-free assay)
~1.8 nM
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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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.
Cell Assay:

[1]
  • Cell lines

    MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3

  • Concentrations

    Dissolved in absolute ethanol, final concentrations ~10 μM

  • Incubation Time

    96 hours

  • Method

    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.
Animal Study:

[1]
  • Animal Models

    Inbred virgin female (Ludwig/Wistar/Olac) rats bearing tumors induced with NMU

  • Dosages

    ~5 mg/kg/day

  • Administration

    Injection s.c.

Customer Product Validation

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]

, 2010, Dr. Zhang of Tianjin Medical University

Selleck's TSA (Trichostatin A) has been cited by 274 publications

Glucocorticoids increase adiposity by stimulating Krüppel-like factor 9 expression in macrophages [ Nat Commun, 2024, 15(1):1190] PubMed: 38331933
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
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
Propionate functions as a feeding-state-dependent regulatory metabolite to counter pro-inflammatory signaling linked to nutrient load and obesity [ J Leukoc Biol, 2024, qiae006] PubMed: 38207130
Pharmaceutical Approach to Develop Novel Photosensitizer Nanoformulation: An Example of Design and Characterization Rationale of Chlorophyll α Derivative [ Pharmaceutics, 2024, 16(1)126] PubMed: 38258135
HDAC1/2/3 are major histone desuccinylases critical for promoter desuccinylation [ Cell Discov, 2023, 9(1):85] PubMed: 37580347
SCARB2 drives hepatocellular carcinoma tumor initiating cells via enhanced MYC transcriptional activity [ Nat Commun, 2023, 14(1):5917] PubMed: 37739936
SCARB2 drives hepatocellular carcinoma tumor initiating cells via enhanced MYC transcriptional activity [ Nat Commun, 2023, 14(1):5917] PubMed: 37739936
Histone 4 lysine 5/12 acetylation enables developmental plasticity of Pristionchus mouth form [ Nat Commun, 2023, 14(1):2095] PubMed: 37055396

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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