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Tubastatin A Hydrochloride

Catalog No. T6161   CAS 1310693-92-5
Synonyms: TSA HCl, Tubastatin A HCl

Tubastatin A Hydrochloride (TSA HCl) is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (<1000-fold) against all other isozymes except HDAC8 (<57-fold).

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Tubastatin A Hydrochloride Chemical Structure
Tubastatin A Hydrochloride, CAS 1310693-92-5
Pack Size Availability Price/USD Quantity
5 mg In stock $ 45.00
10 mg In stock $ 53.00
25 mg In stock $ 68.00
50 mg In stock $ 77.00
100 mg In stock $ 126.00
200 mg In stock $ 207.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.25%
Purity: 97.55%
Purity: 97.24%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tubastatin A Hydrochloride (TSA HCl) is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (>1000-fold) against all other isozymes except HDAC8 (>57-fold).
Targets&IC50 HDAC6:15 nM
In vitro Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. [1] Tubastatin A increases Foxp3+ T-regulatory cells (Tregs) suppression of T cell proliferation at 100 ng/mL in vitro. [2] Tubastatin A treatment in C2C12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes. [3] A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L. [4]
In vivo Daily treatment of 0.5 mg/kg Tubastatin A inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, which including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection. [2]
Kinase Assay Enzyme Inhibition Assays: Enzyme inhibition assays are performed by the Reaction Biology Corporation, Malvern, PA, using the Reaction Biology HDAC Spectrum platform. (www.reactionbiology.com) The HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays use isolated recombinant human protein; HDAC3/NcoR2 complex is used for the HDAC3 assay. Substrate for HDAC1, 2, 3, 6, 10, and 11 assays is a fluorogenic peptide from p53 residues 379-382 (RHKKAc); substrate for HDAC8 is fluorogenic diacyl peptide based on residues 379-382 of p53 (RHKAcKAc). Acetyl-Lys (trifluoroacetyl)-AMC substrate is used for HDAC4, 5, 7, and 9 assays. Tubastatin A is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 30 μM. Control Compound Trichostatin A (TSA) is tested in a 10-dose IC50 with 3-fold serial dilution starting at 5 μM. IC50 values are extracted by curve-fitting the dose/response slopes.
Cell Research Primary cortical neuron cultures are obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. All experiments are initiated 24 hours after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells are rinsed with warm PBS and then placed in minimum essential medium (Invitrogen) containing 5.5 g/L glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine. Oxidative stress is induced by the addition of the glutamate analogue homocysteate (HCA; 5 mM) to the media. HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. In combination with HCA, neurons are treated with Tubastatin A at the indicated concentrations. Viability is assessed after 24 hours by MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method.(Only for Reference)
Synonyms TSA HCl, Tubastatin A HCl
Molecular Weight 371.86
Formula C20H21N3O2·HCl
CAS No. 1310693-92-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.7 mg/mL (10 mM), with gentle warming

TargetMolReferences and Literature

1. Butler KV, et al, J Am Chem Soc, 2010, 132(31), 10842-10846. 2. de Zoeten EF, et al, Mol Cell Biol, 2011, 31(10), 2066-2078. 3. Di Fulvio S, et al, PloS One, 2011, 6(12):e28563. 4. Ketene AN, et al, Integr Biol (Camb), 2012, 4(5), 540-549.

TargetMolCitations

1. Liu S, Zhang H L, Li J, et al.Tubastatin A potently inhibits GPX4 activity to potentiate cancer radiotherapy through boosting ferroptosis.Redox Biology.2023: 102677.

Related compound libraries

This product is contained In the following compound libraries:
Epigenetics Compound Library Anti-Cancer Compound Library Inhibitor Library Reprogramming Compound Library Histone Modification Compound Library Autophagy Compound Library Bioactive Compound Library Target-Focused Phenotypic Screening Library NF-κB Signaling Compound Library Cancer Cell Differentiation Compound Library

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Keywords

Tubastatin A Hydrochloride 1310693-92-5 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Tubastatin A Histone deacetylases Inhibitor inhibit TSA HCl Tubastatin A HCl inhibitor

 

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