Tubastatin A

SKU: orb1306944

Description

Tubastatin A is a potent and highly selective HDAC6 inhibitor, exhibiting an IC50 of 15 nM in biochemical assays with >1000-fold selectivity over other HDAC isoforms except HDAC8. It is widely used in both in vitro and in vivo research to investigate HDAC6's role in oncology, neurology, and immunology, including studies on neurodegenerative disease models and cancer cell proliferation.

Research Area

Cell Biology, Epigenetics & Chromatin, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 1252003-15-8
• MW: 335.4
• Purity: 97.22% (May vary between batches)
• Formula: C₂₀H₂₁N₃O₂
• SMILES: CN1CCc2c(C1)c1ccccc1n2Cc1ccc(cc1)C(=O)NO
• Target: Antibacterial,HDAC,Apoptosis,Autophagy
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:35 mg/mL (104.35 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.98 mM)

Bioactivity

• Target IC50:
  HDAC8:854 nM|HDAC6:15 nM|HDAC1:16400 nM
• In Vivo:
  Tubastatin A (5 μM) dose-dependently protected neuronal cells from homocysteine-induced death, which was completely avoided at 10 μM. Tubastatin A (10 μM) slightly induced histone acetylation. When applied to cholangiocarcinoma cell lines, Tubastatin A (10 μM) induced an increase in the level of acetylated α-tubulin and the restoration of primary cilia expression, which correlated with the down-regulation of Hedgehog and MAPK signaling pathways, and a decrease in the rate of cell proliferation (50% on average) and infiltration (40%). Tubastatin A significantly inhibited TNF-α and IL-6 when acting on lipopolysaccharide-stimulated human THP-1 macrophages (IC50: 272/712 nM). When acting on mouse Raw 264.7 macrophages, Tubastatin A dose-dependently inhibited nitric oxide secretion (IC50: 4.2 μM).
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• In Vitro:
  Tubastatin A (5 μM) dose-dependently protected neuronal cells from homocysteine-induced death, which was completely avoided at 10 μM. Tubastatin A (10 μM) slightly induced histone acetylation. When applied to cholangiocarcinoma cell lines, Tubastatin A (10 μM) induced an increase in the level of acetylated α-tubulin and the restoration of primary cilia expression, which correlated with the down-regulation of Hedgehog and MAPK signaling pathways, and a decrease in the rate of cell proliferation (50% on average) and infiltration (40%). Tubastatin A significantly inhibited TNF-α and IL-6 when acting on lipopolysaccharide-stimulated human THP-1 macrophages (IC50: 272/712 nM). When acting on mouse Raw 264.7 macrophages, Tubastatin A dose-dependently inhibited nitric oxide secretion (IC50: 4.2 μM).
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• Cell Research:
  Anchorage-independent growth is assessed by growing cells in soft agar. About 25,000 cells suspended in 0.4% agar in culture media are layered over a 1% agar layer in a 6-well plate. Media are added twice a week and pictures are taken after 21 days of incubation. The number and size of colonies are analyzed using the Gel-Pro software.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tubastatin A, Tubastatin A BASE, Apoptosis, Autophagy, HDAC, HDAC6, Histone deacetylases

Compound Identifiers

PubChem CID

49850262