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.

• Synonym(e): HDAC Inhibitor XXIII, Tubastatin A, N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide
• Empirische Formel (Hill-System): C₂₀H₂₁N₃O₂
• Molekulargewicht: 335.40
• UNSPSC-Code: 12352200
• NACRES: NA.28

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic); protect from light
• Farbe: tan
• Löslichkeit: DMSO: 10 mg/mL; ethanol: 250 μg/mL
• Versandbedingung: ambient
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable