Tubastatin A HCl (Synonyms: TSA HCl;Tubastatin A hydrochloride) |
| Catalog No.GC10322 |
Tubastatin A HCl (Tubasatin A HCl) est un inhibiteur puissant et sélectif de HDAC6 avec une IC50 de 15 nM dans un test acellulaire, et est sélectif (1000 fois plus) contre toutes les autres isozymes sauf HDAC8 (57 fois plus). Tubastatine A HCl inhibe également HDAC10 et métallo-β-lactamase contenant la protéine2 (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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