Tubastatin A

SKU: orb1226676

Description

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in cell-free assays; displays 57-fold selectivity over HDAC8 and >1,000-fold selective against other HDAC isoforms; induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines at 10 uM, shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with IC50 of 272 nM and 712 nM; reduces the growth of cholangiocarcinoma in vivo.

Key Properties

• CAS Number: 1252003-15-8
• MW: 335.4
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₁N₃O₂
• SMILES: CN1CCC2=C(C1)C1=CC=CC=C1N2CC1=CC=C(C=C1)C(=O)NO
• Target: HDAC
• Solubility: DMSO: ≥ 45 mg/mL

Bioactivity

• In Vivo:
  Daily treatment of Tubastatin A at 0.5 mg/kg inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection.
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• In Vitro:
  Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. At 100 ng/mL Tubastatin A increases Foxp3+ T-regulatory cells (Tregs) suppression of T cell proliferation in vitro. Tubastatin A treatment in CC12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes. A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

HDAC