Tubastatin A HCl (Synonyms: TSA HCl;Tubastatin A hydrochloride) |
| Catalog No.GC10322 |
Tubastatin A HCl (Tubastatin A HCl) es un inhibidor potente y selectivo de HDAC6 con IC50 de 15 nM en un ensayo libre de células, y es selectivo (1000 veces mÁs) contra todas las demÁs isoenzimas excepto HDAC8 (57 veces mÁs). Tubastatin A HCl también inhibe HDAC10 y metalo-β-proteÍna 2 que contiene el dominio de lactamasa (MBLAC2).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1310693-92-5
Sample solution is provided at 25 µL, 10mM.
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Tubastatin A HCl is a selective inhibitor of HDAC6 with IC50 value of 15 nM [1].
HDAC6 (histone deacetylase 6) is an enzyme and plays an important role in a variety of processes, including transcriptional regulation, cell cycle preogression and developmental events. Abnormal expression of HDAC6 is correlated with many kinds of diseases, including Alzheimer's disease and cancers [1].
Tubastatin A HCl is a potent HDAC6 inhibitor and has the most selective compared with other HDAC isoforms. When tested with primary cortical neuron cells, Tubastatin A HCl treatment protected HCA-induced neuronal cell death in a dose range from 5 μM to 10 μM [1]. In HaCaT cells, administration of Tubastatin A HCl prevented sodium arsenite from inducing association of Nrf2 mRNA with ribosomes and elevation of Nrf2 protein by selectively inhibitng HDAC6 activity and had no effect on other HDACs [2]. Using atomic force microscopy study, Ketene AN et al. revealed that Tubastatin A HCl increased cell elasticity by inhibiting HDAC6 [3].
References:
[1]. Kyle V. Butler, Jay Kalin, Camille Brochier, et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A [J]. J. Am. Chem. Soc., 2010, 132 (31), pp 10842–10846.
[2]. Kappeler KV, Zhang J, Dinh TN, et al. Histone deacetylase 6 associates with ribosomes and regulates de novo protein translation during arsenite stress [J]. Toxicol Sci. 2012 May;127(1):246-255.
[3]. Ketene AN, Roberts PC, Shea AA, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells [J]. Integr Biol (Camb). 2012 May;4(5):540-549.
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