Tubastatin A HCl

Tubastatin A HCl

Catalog Number:
L002369607APE
Mfr. No.:
APE-A8547
Price:
$196
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          TSA HCl;Tubastatin A hydrochloride; N-hydroxy-4-[(2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)methyl]benzamide;hydrochloride
          CAS Number
          1310693-92-5
          Molecular Formula
          C20H21N3O2·HCl
          Molecular Weight
          371.86
          Appearance
          A solid
          Purity
          98.78%
          Solubility
          insoluble in EtOH; ≥12.34 mg/mL in H2O; ≥18.6 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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