Tubacin

SKU: orb1300866

Description

Tubacin is a potent, reversible, and cell-permeable small molecule that selectively inhibits HDAC6 with a 4 nM IC50, showing ~350-fold selectivity against HDAC1. It is widely used in vitro and in vivo to study HDAC6's role in oncology, neurology, and immunology, particularly in processes involving protein aggregation and cell motility.

Research Area

Epigenetics & Chromatin, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 537049-40-4
• MW: 721.86
• Purity: 98.71% (May vary between batches)
• Formula: C₄₁H₄₃N₃O₇S
• SMILES: S(C[C@@H]1O[C@@H](O[C@@H](C1)C2=CC=C(CO)C=C2)C3=CC=C(NC(CCCCCCC(NO)=O)=O)C=C3)C4=NC(=C(O4)C5=CC=CC=C5)C6=CC=CC=C6
• Target: HDAC|||Virus Protease
• Solubility: H2O:<1 mg/mL;DMSO:50 mg/mL (69.27 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (4.57 mM);Ethanol:<1 mg/mL

Bioactivity

• Target IC50:
  HDAC4:17.30 μM|HDAC1:1.40 μM|HDAC2:6.27 μM|HDAC7:9.70 μM|HDAC5:3.35 μM|HDAC9:4.31 μM|HDAC8:1.27 μM|HDAC10:3.71 μM|HDAC6 (cell-free assay):4nM|HDAC11:3.79 μM|HDAC3:1.27 μM
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• In Vivo:
  In chick embryos, inhibition of HDAC6 activity by Tubacin reduces the formation of new blood vessels in matrigel/nylon mesh. In angioreactors implanted in mice, Tubacin also impairs the formation of new blood vessels.
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• In Vitro:
  Tubacin, without directly stabilizing microtubules, induces an increase in α-tubulin acetylation with EC50 of 2.5 μM in A549 cells. Tubacin inhibits HDAC6-mediated α-tubulin deacetylation, and inhibits the migration of both wild-type and HDAC6-overexpressing cells. Tubacin, in combination with paclitaxel, synergistically enhances tubulin acetylation. Tubacin significantly inhibits both drug-sensitive and drug–resistant MM cell growth with IC50 of 5–20 μM, and induces cell apoptosis by activation of caspases.
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• Cell Research:
  Cell lines: Drug-sensitive (MM.1S,U266,INA-6,and RPMI8226) and drug-resistant (RPMI-LR5 and RPMI-Dox40) MM cell lines. Concentrations: ~20 μM. Incubation Time: 72 hours. Method:The inhibitory effect of bortezomib and/or tubacin on MM cell growth is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye absorbance.All experiments are performed in quadruplicate.
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• Animal Research:
  Animal Models: Athymic nude mice implanted with angioreactorsFormulation: DMSODosages: --Administration: Tubacin is filled in semiclosed angioreactors, and then implanted into the mice.
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Storage & Handling

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

Alternative Names

inhibit, Inhibitor, HDAC, HDAC6, Histone deacetylases, VirusProtease, Virus Protease, Tubacin

Compound Identifiers

PubChem CID

6675804