HD-75 is an isoxazole-based compound which acts as a photoreactive histone deacetylase (HDAC) inhibitor suitable for photoaffinity labeling experiments. This allows for the identification of drug target proteins of biologically active compounds and mapping their binding sites.
HD-75 specifically inhibits HDAC3, showing a 9-fold selectivity versus HDAC8. Cell-based studies show HD-75 is able to freely enter the cell nucleus and trigger mechanisms known to respond to HDAC inhibition such as accumulation of acetylated H4, activation of caspase 3, and cell death of highly proliferative human cancer cell lines at low micromolar concentrations. Additionally, unlike SAHA, HD-75, does not exert cytotoxic effect in neuronal-like cells and even protected these cells from chemically induced apoptosis.
From the laboratory of Pavel A. Petukhov, PhD, University of Illinois at Chicago.
Part of The Investigator's Annexe program.
|Product Type:||Small Molecule|
|Stability:||> 6 months when stored at -20C|
|Comments:||Photoreactive group: arylazide; Activation wavelength: 280nm; Activation period: 3min|
|Storage:||Store at -20C|
|Compound||IC50 ± SD (nM)||HDAC8/HDAC3|
|SAHA||27 ± 1.0||440 ± 21||16.3|
|HD-75||73 ± 15||707 ± 86||9.68|
Adapted from Table 1; Neelarapu, R., et al. Journal of Medicinal Chemistry. 54: 4350 - 4364. 2011.
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