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382187 Sigma-Aldrich

HDAC Inhibitor XXIII, Tubastatin A - Calbiochem

The HDAC Inhibitor XXIII, Tubastatin A controls the biological activity of HDAC. This small molecule/inhibitor is primarily used for Cell Structure applications.

Synonym: N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide, N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide

  • Empirical Formula (Hill Notation) C20H21N3O2

  • Molecular Weight 335.40

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Properties

Related Categories Biochemicals and Reagents, D to K, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates,
brand family   Calbiochem
feature productdata solubility   DMSO (10 mg/ml) or Ethanol (250 µg/ml)
form   Tan solid
packaging   5 mg in Glass bottle (382187-5MG)
purity   ≥95% by HPLC
shipped in   ambient
storage conditions   -20C
  Hygroscopic
  Ok to freeze
  Protect from light

Description

General description

A cell-permeable carbazolohydroxamate that acts as a highly potent HDAC6-selective inhibitor (IC50 = 15 nM) with much reduced or no activity against other known HDACs. Effectively prevents neuronal cell death (by ≥95% at 10 µM) upon oxidative stress induction by HCA and selectively induces cellular α-tubulin, but not histone H4, hyperacetylation (2.5 to 5 µM) in primary rat cortical neuron cultures.

A cell-permeable carbazolohydroxamate whose zinc-chelating hydroxamic acid moiety and catalytic channel rim-targeting aromatic cap structure render it a highly potent HDAC6-selective inhibitor (IC50 = 15 nM against recombinant human HDAC6) with much reduced or no activity against HDAC8, HDAC1 (IC50 = 0.854 and 16.4 µM, respectively), and other known HDACs (HDAC2/3/4/5/7/9/10/11; IC50 >30 µM). Shown to selectively block HDAC6-, but not HDAC1-, dependent cellular deacetylation as evidenced by its selective induction (2.5 to 5 µM) of α-tubulin, but not histone H4, hyperacetylation in cultured primary rat cortical neurons. Although failing to block cellular glutathione depletion by homocysteic acid (HCA), Tubastatin A nevertheless is reported to prevent neuronal cell death upon oxidative stress induction by HCA in a dose-dependent manner (≥95% protection at 10 µM), presumably by preventing peroxiredoxins deacetylation.

Other Notes

Butler, K.V., et al. 2010. J. Am. Chem. Soc.132, 10842.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Standard Handling (A)

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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