Trichostatin A (TSA)
Trichostatin A (TSA) is a potent inhibitor of histone deacetylase (HDAC) as well as an antifungal antibiotic with cytostatic and differentiating properties that noncompetivively and reversibly inhibits HDAC, at low nanomolar concentrations, in both cultured mammalian cells and fractionated cell nuclear extracts. It is capable of arresting cells in G1 and G2 phases of the cell cycle, inducing differentiation and reverting the transformed morphology of cells in culture. According to a study investigating the effect of TSA in human breast cancer cell lines, TSA inhibited proliferation of breast carcinoma cell lines (IC50 124.4 ± 120.4 nM), comparing to all cell lines (IC50 2.4 ± 0.5 nM), and resulted in pronounced histone H4 hyperacetylation.
Reference
David M. Vigushin, Simak Ali, Paul E. Pace, Nina Mirsaidi, Kazuhiro Ito, Ian Adcock, and R. Charles Coombes. Trichostatin A is a histone deacetylase inhibitor with potent antitumot activity against breast cancer in vivo. Clin Cancer Res 2001;7:971-976
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| Storage | Desiccate at -20°C |
| M.Wt | 302.37 |
| Cas No. | 58880-19-6 |
| Formula | C17H22N2O3 |
| Synonyms | Trichostatin A,TSA |
| Solubility | insoluble in H2O; ≥15.12 mg/mL in DMSO; ≥16.56 mg/mL in EtOH with ultrasonic |
| Chemical Name | (2E,4E,6R)-7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C=C(C)C=CC(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment[1]: | |
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Cell lines |
Human breast cancer cell line |
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Preparation method |
The solubility of this compound in DMSO is |
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Reaction Conditions |
10 μM TSA solved in growth medium containing 0.1% (v/v) ethanol for 96 h incubation |
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Applications |
TSA inhibited proliferation of eight breast carcinoma cell lines with mean ± SD IC50 of 124.4 ± 120.4 nM (range, 26.4–308.1 nM). TSA treatment resulted in pronounced histone H4 hyperacetylation. |
| Animal experiment [1]: | |
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Animal models |
Inbred virgin female (Ludwig/Wistar/Olac) rats bearing tumors induced with NMU |
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Dosage form |
500 μg/kg by injection daily for 4 weeks |
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Applications |
TSA had pronounced antitumor activity in vivo. that The antitumor activity of TSA attributabled to induction of differentiation. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Vigushin DM1, Ali S, Pace PE et al. Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo. Clin Cancer Res. 2001 Apr;7(4):971-6. |
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| Targets | HDAC | |||||
| IC50 | ~1.8 nM |
Quality Control & MSDS
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