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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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Purity: ≥98%
Trichostatin A (also called TSA) is a novel, potent and specific inhibitor of histone deacetylase (HDAC) with potential anticancer activity. Its IC50 value for HDAC inhibition is 1.8 nM. Additionally, at low nanomolar concentrations, it reversibly and noncompetivively inhibits HDAC in both fractionated cell nuclear extracts and cultured mammalian cells. It possesses cytostatic and differentiating qualities as an antifungal antibiotic agent. A study looking at TSA's impact on human breast cancer cell lines found that TSA significantly increased histone H4 hyperacetylation and inhibited the proliferation of breast carcinoma cell lines (IC50 124.4 ± 120.4 nM) compared to all other cell lines (IC50 2.4 ± 0.5 nM).
Targets |
HDAC ( IC50 = 1.8 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Each of the following breast cancer cell lines is used to prepare total cellular extracts: 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) is 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. These conditions are followed by different concentrations of Trichostatin A in 0.1% (v/v) ethanol or 0.1% (v/v) ethanol as vehicle control. Scintillation counting is used to quantify the released [3H]acetate after each 200 μL reaction is extracted with 600 μL of ethyl acetate and quenched with 50 μL of 1 M HCl/0.16 M acetic acid. In order to fit inhibition data to the appropriate dose-response curve, IC50 values are graphically determined using nonlinear regression.
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Cell Assay |
For 72 hours, cells are cultivated in a 96-well plate at a density of 1×103 cells per well using 100 μL of full-dose DMEM, either with or without the HDAC inhibitor Trichostatin A. With a CCK-8 cell proliferation kit, the WST-8 assay is used to quantify cytotoxicity. A microplate reader is used to measure the absorbance at 450 nm. Three separate experiments are conducted, and each experiment is run in triplicate.
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Animal Protocol |
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References |
Molecular Formula |
C17H22N2O3
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Molecular Weight |
302.4
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Exact Mass |
302.16
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Elemental Analysis |
C, 67.53; H, 7.33; N, 9.26; O, 15.87
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CAS # |
58880-19-6
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Appearance |
Solid powder
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SMILES |
C[C@H](/C=C(\C)/C=C/C(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C
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InChi Key |
RTKIYFITIVXBLE-QEQCGCAPSA-N
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InChi Code |
InChI=1S/C17H22N2O3/c1-12(5-10-16(20)18-22)11-13(2)17(21)14-6-8-15(9-7-14)19(3)4/h5-11,13,22H,1-4H3,(H,18,20)/b10-5+,12-11+/t13-/m1/s1
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Chemical Name |
(2E,4E,6R)-7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3069 mL | 16.5344 mL | 33.0688 mL | |
5 mM | 0.6614 mL | 3.3069 mL | 6.6138 mL | |
10 mM | 0.3307 mL | 1.6534 mL | 3.3069 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.