The HDAC Inhibitor XXIII, Tubastatin A controls the biological activity of HDAC. This small molecule/inhibitor is primarily used for Cell Structure applications.
Synonim(y):
HDAC Inhibitor XXIII, Tubastatin A, N-Hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide
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OK to freeze desiccated (hygroscopic) protect from light
kolor
tan
rozpuszczalność
DMSO: 10 mg/mL ethanol: 250 μg/mL
Warunki transportu
ambient
temp. przechowywania
−20°C
Opis ogólny
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.
Opakowanie
Packaged under inert gas
Ostrzeżenie
Toxicity: Standard Handling (A)
Rekonstytucja
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Inne uwagi
Butler, K.V., et al. 2010. J. Am. Chem. Soc.132, 10842.
Informacje prawne
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 2
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
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