TUBASTATIN A

Background Information:

Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM.
Comparatively, it demonstrates over 1,000-fold selectivity against all
other HDAC isoforms (IC50s >16 μM), excluding HDAC8 (IC50 = 0.9 μM).
Tubastatin A induces α-tubulin hyperacetylation at 2.5 μM in primary
cortical neuron cultures. In a model of oxidative stress induced by
glutathione depletion, tubastatin A displays dose-dependent neuronal
protection of primary cortical neuron cultures at 5-10 μM.

Reference:

1. Butler KV, Kalin J, Brochier C, Vistoli G, Langley B, Kozikowski
AP. Rational design and simple chemistry yield a superior,
neuroprotective HDAC6 inhibitor, tubastatin A. J Am Chem Soc. 2010 Aug
11;132(31):10842-6.
2. Our in-house head-to-head assay for ChemieTek’s three HDAC6
inhibitors, Tubacin, Tubastatin A and Compound 7, has yielded IC50s of
5, 7 and 4 nM, respectively.

APIM050344: TUBASTATIN A

CAS No.: 1310693-92-5.
Molecular Formula: C₂₀H₂₁N₃O₂?HCl ? 0.4H₂O.
Molecular Weight: 379.1.
Purity: 99.5% (HPLC at 215 nm and 254 nm).
QC: HPLC- MS, ¹HNMR, and Elemental Analysis Report.
Solubility: Soluble in Water, DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.