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TSA (Trichostatin A)

TSA (Trichostatin A)

Item no.	S1045-5
Manufacturer	Selleckchem
CASRN	58880-19-6
Amount	5 mg
Quantity options	10 mg 1 g 10 g 100 mg 10 mM/1 mL 2 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Aging & Neurological Disorders Neural Epigenetics Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer
Type	Inhibitors
Specific against	other
Smiles	CC(C=C(C)C=CC(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	HDAC,HDAC
Similar products	Trichostatin
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	302, 4
Administration	Injection s.c.
Animal Models	Inbred virgin female (Ludwig/Wistar/Olac) rats bearing tumors induced with NMU
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 ca.10 uM
Dosages	ca.5 mg/kg/day
Formulation	Dissolved in DMSO
IC50	ca.1.8 nM [1], ca.1.8 nM [1], ca.1.8 nM [1], ca.1.8 nM [1], ca.1.8 nM [1], ca.1.8 nM [1]
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 ERalpha than the ERalpha-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 beta type II receptor (TbetaRII) 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 TbetaRII 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]
Incubation Time	96 hours
Kinase Assay	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 uL crude cell extract (ca.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 uL (ca.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 uL reaction is quenched with 50 uL of 1 M HCl/0.16 M acetic acid and extracted with 600 uL 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.
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.
Solubility (25C)	DMSO 23 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	TSA (Trichostatin A) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Chemical Name	(R, 2E, 4E)-6-(4-(dimethylamino)benzoyl)-N-hydroxy-4-methylhepta-2, 4-dienamide

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S1045-5-datasheet.pdf

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