5.08194

HDAC6 Inhibitor III

• Synonym(s): HDAC6 Inhibitor III
• Empirical Formula (Hill Notation): C₂₀H₁₉N₃O₃
• CAS Number: 1450618-49-1
• Molecular Weight: 349.38
• UNSPSC Code: 12352200

Properties

• assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• potency: 29 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: cream
• solubility: DMSO: 10 mg/mL
• storage temp.: −20°C

Description

General description

A cell-permeable, quinazolin-4-one based hydroxamic acid containing compound that acts as a potent and selective inhibitor of histone deacetylase 6 (HDAC6; IC₅₀ = 29 nM). Exhibits high selectivity over other HDACs (IC₅₀ = 1.88, 6.45, 1.75, and 4.08 µM for HDAC1, 2, 8, and 11, respectively). Does not affect hERG activity (>10 µM) or p450 activity (IC₅₀ >6.5 µM). Blocks b-amyloid (Ab) aggregation in the presence of zinc (IC₅₀ = 9.5 µM) and improves learning-based performance in mice. Induces neurite outgrowth (EC₅₀ = 7.3 and 9.2 µM in PC12 and SH-SY5Y cells, respectively) and enhances synaptic activity (EC₅₀ = 6.5 and 6.8 µM in PC12 and SH-SY5Y cells, respectively). Shown to enhance acetylated a-tubulin levels in hippocampus region of mice with Ab lesions.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Yu, C.W., et al. 2013. J. Med. Chem.56, 6775.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable