382187

HDAC Inhibitor XXIII, Tubastatin A

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

• Synonyme(s) : HDAC Inhibitor XXIII, Tubastatin A, N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide
• Formule empirique (notation de Hill): C₂₀H₂₁N₃O₂
• Poids moléculaire : 335.40
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.28

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: tan
• Solubilité: DMSO: 10 mg/mL; ethanol: 250 μg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable