Tubastatin A Hydrochloride

SKU: orb1301022

Description

Tubastatin A Hydrochloride is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM, demonstrating over 1000-fold selectivity against other HDACs except HDAC8. It is widely used in research to study HDAC6's role in cellular processes, including neurobiology and oncology, in both in vitro and in vivo experimental models.

Research Area

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

Key Properties

• CAS Number: 1310693-92-5
• MW: 371.86
• Purity: 99.25% (May vary between batches)
• Formula: C₂₀H₂₁N₃O₂·HCl
• SMILES: Cl.CN1CCc2c(C1)c1ccccc1n2Cc1ccc(cc1)C(=O)NO
• Target: Autophagy,HDAC,Antibacterial,Apoptosis
• Solubility: H2O:7.43 mg/mL (19.98 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.69 mM);DMSO:3.76 mg/mL (10.11 mM)

Bioactivity

• Target IC50:
  HDAC8:854 nM|HDAC6:15 nM|HDAC1:16400 nM
• In Vivo:
  Daily administration of 0.5 mg/kg Tubastatin A inhibits HDAC6, enhancing Tregs suppressive activity in mouse models of inflammation and autoimmunity, including various forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection.
• In Vitro:
  Tubastatin A exhibits high selectivity for all 11 HDAC isoforms, demonstrating over 1000-fold selectivity compared to all but HDAC8, for which it shows approximately 57-fold selectivity. In assays measuring neurodegeneration induced by homocysteic acid (HCA), Tubastatin A offers dose-dependent neuroprotection, achieving near-complete protection at concentrations of 10 μM, starting from 5 μM. Further, at a dosage of 100 ng/mL in vitro, it enhances the suppression of T cell proliferation by Foxp3+ T-regulatory cells (Tregs). In C2C12 cells, treatment with Tubastatin A disrupts myotube formation by causing early hyperacetylation of alpha-tubulin during the myogenic process, though it permits myotube elongation when hyperacetylation occurs within the myotubes. Additionally, recent studies have shown that Tubastatin A increases cell elasticity in mouse ovarian cancer cell lines, MOSE-E and MOSE-L, as determined by atomic force microscopy (AFM), without significantly altering the actin microfilament or microtubule networks.
• Cell Research:
  Primary cortical neuron cultures are obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. All experiments are initiated 24 hours after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells are rinsed with warm PBS and then placed in minimum essential medium (Invitrogen) containing 5.5 g/L glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine. Oxidative stress is induced by the addition of the glutamate analogue homocysteate (HCA; 5 mM) to the media. HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. In combination with HCA, neurons are treated with Tubastatin A at the indicated concentrations. Viability is assessed after 24 hours by MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tubastatin A, Tubastatin A HCl, Tubastatin A Hydrochloride, TSA HCl, Autophagy, Apoptosis, Histone deacetylases, HDAC1, HDAC, HDAC6, HDAC3, HDAC2, HDAC8, Inhibitor, inhibit

Compound Identifiers

PubChem CID

57336514