A8183-5mg | Trichostatin A (TSA) [58880-19-6] Quimigen Portugal

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

1. Min Yang, et al. "Trichostatin A enhances the titanium rods osseointegration in osteoporotic rats by the inhibition of oxidative stress through activating the AKT/Nrf2 pathway." Sci Rep. 2023 Dec 27;13(1):22967. PMID: 38151509
2. Haitao Wen, Jianwen Chen, et al. "Repression of ferroptotic cell death by mitochondrial calcium signaling." Res Sq. 2023 Jul 10;rs.3.rs-3029860. PMID: 37502961
3. Joseph Boyle, Derick Chiappo, et al. "Aminocoumarin-based heme oxygenase activity fluorescence probe reveals novel aspects of HO-1 regulation." Research Square. 22 Nov, 2023.
4. Zhang J, Ouyang Z, et al. "Dynamic chromatin landscape encodes programs for perinatal transition of cardiomyocytes." Cell Death Discov 2023 Jan 18;9(1). PMID: 36653336
5. Yoichiro Kawamura, Lingyang Hua, et al. "Histone deacetylase inhibitors enhance oncolytic herpes simplex virus therapy for malignant meningioma." Biomed Pharmacother. 2022 Nov;155:113843. PMID: 36271587
6. Jan Zimak, Zachary W Wagoner, et al. "Epigenetic silencing directs expression heterogeneity of stably integrated multi-transcript unit genetic circuits." Sci Rep. 2021 Jan 28;11(1):2424. PMID: 33510302
7. Tianliang Li, Ligang Kong, et al. "Listeria monocytogenes upregulates mitochondrial calcium signalling to inhibit lc3-associated phagocytosis as a survival strategy." Nat Microbiol. 2021 Mar;6(3):366-379. PMID: 33462436
8. Somayeh Layeghi-Ghalehsoukhteh, Shreoshi Pal Choudhuri, et al. "Concerted cell and in vivo screen for pancreatic ductal adenocarcinoma (PDA) chemotherapeutics." Sci Rep. 2020 Nov 26;10(1):20662. PMID: 33244070
9. Haiyang Yu, Shan Lu, et al. "TDP-43 and HSP70 phase separate into anisotropic, intranuclear liquid spherical annuli." bioRxiv. March 29, 2020.
10. Xu W, Huang M, et al. "The Role of CHK1 Varies with the Status of Oestrogen-receptor and Progesterone-receptor in the Targeted Therapy for Breast Cancer." Int J Biol Sci. 2020;16(8):1388-1402. PMID: 32210727
11. Tang Y, Yu W. "SIRT1 and p300/CBP regulate the reversible acetylation of serine-threonine kinase NDR2." Biochem Biophys Res Commun. 2019 Aug 16. pii: S0006-291X(19)31586-4. PMID: 31427083
12. Dhana Friedrich, Laura Friedel, et al. "Stochastic transcription in the p53-mediated response to DNA damage is modulated by burst frequency." bioRxiv. 2019 June 21.
13. Wang MH, Wu CH, et al. "Nerve-mediated expression of histone deacetylases regulates limb regeneration in axolotls." Dev Biol. 2019 May 15;449(2):122-131. PMID: 30826398
14. Zheng Q, Liu P, et al. "Mitochondrion-processed TERC regulates senescence without affecting telomerase activities." Protein Cell. 2019 Feb 20. PMID: 30788732
8. Sheridan J.S. Carrington. "Differential Glycosylation of the Inwardly Rectifying Potassium Channel Kir7.1 by G protein-coupled Receptors." Vanderbilt University. 2019.
16. Ling H, Peng L, et al. "Histone Deacetylase SIRT1 Targets Plk2 to Regulate Centriole Duplication." Cell Rep. 2018 Dec 4;25(10):2851-2865.e3. PMID: 30517871
17. Jiang H, Zhang S, et al. "Trichostatin a Protects Dendritic Cells Against Oxygen-Glucose Deprivation via the SRSF3/PKM2/Glycolytic Pathway." Front Pharmacol. 2018 Jun 11;9:612. PMID: 29942258
18. Prasad H, Rao R. "Histone deacetylase-mediated regulation of endolysosomal pH." J Biol Chem. 2018 Mar 22. pii: jbc.RA118.002025. PMID: 29567836
19. Choi S, Uehara H, et al. "RNA activating-double stranded RNA targeting flt-1 promoter inhibits endothelial cell proliferation through soluble FLT-1 upregulation." PLoS One. 2018 Mar 6;13(3):e0193590. PMID: 29509796
20. Rajini Rao, Hari Prasad. "A conserved mechanism for regulation of endo-lysosomal pH by histone deacetylases." bioRxiv. 2018 January 22.
21. Hari Prasad, Rajini Rao. "The Amyloid Clearance Defect in ApoE4 Astrocytes is Corrected by Epigenetic Restoration of NHE6." bioRxiv. 2018.January. 4
22. Yan Y, Wang H, et al. "HDAC6 Suppresses Age-Dependent Ectopic Fat Accumulation by Maintaining the Proteostasis of PLIN2 in Drosophila." Dev Cell. 2017 Oct 9;43(1):99-111.e5. PMID: 28966044
23. Hai Y, Shinsky SA, et al. "Histone deacetylase 10 structure and molecular function as a polyamine deacetylase." Nat Commun. 2017 May 18;8:15368. PMID: 28516954
24. Mitani Y, Vagnozzi RJ, Millay DP. "In vivo myomaker-mediated heterologous fusion and nuclear reprogramming. FASEB J. 2017 Jan;31(1):400-411." PMID: 27825107
25. Cai D, Wang X, et al. "Establishment of an inducible HBV stable cell line that expresses cccDNA-dependent epitope-tagged HBeAg for screening of cccDNA modulators." Antiviral Res. 2016 May 13;132:26-37. PMID: 27185623

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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]:
Cell lines	Human breast cancer cell line
Preparation method	The solubility of this compound in DMSO is
Reaction Conditions	10 μM TSA solved in growth medium containing 0.1% (v/v) ethanol for 96 h incubation
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]:
Animal models	Inbred virgin female (Ludwig/Wistar/Olac) rats bearing tumors induced with NMU
Dosage form	500 μg/kg by injection daily for 4 weeks
Applications	TSA had pronounced antitumor activity in vivo. that The antitumor activity of TSA attributabled to induction of differentiation.
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.
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.

Targets	HDAC
IC50	~1.8 nM

Purity = 98.22%

Trichostatin A (TSA) [58880-19-6]

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