Name | Pyroxamide |
Description | Pyroxamide is an histone deacetylases (HDACs) inhibitor with antineoplastic properties ( HDAC1;IC50: 0.1-0.2 μM). |
Cell Research | HDAC1 enzyme assay, ?A MEL cell line expressing the epitope Flag-tagged HDAC1 was generated.?HDAC1-Flag was affinity purified by immunoprecipitation using M2 anti-Flag antibody-coated agarose, followed by elution from the agarose using the Flag peptide.?[3H]acetate-labeled cellular histones were prepared from MEL cells and were used as a substrate for the HDAC activity assay.?Released [3H]acetic acid was quantified by scintillation counting.?For inhibition studies, the enzyme preparations were preincubated with pyroxamide (10 to 100,000 nm) for 30 min at 4°C.[1] |
In vitro | The activity of pyroxamide as an inhibitor of HDACs.?Pyroxamide inhibited the enzymatic activity of affinity-purified HDAC1 at submicromolar concentrations ?.?The ID50 value for inhibition of HDAC1 activity by pyroxamide was ~100 nm.MEL cells incubated with pyroxamide (4 μm) for 4, 24, or 48 h showed accumulation of acetylated histones H2A, H2B, H3, and H4 .?Cells cultured without the agent had low basal levels of acetylated histones at the same time points[1] |
In vivo | Pyroxamide may be a useful agent for the treatment of malignancy and that induction of p21/WAF1 in transformed cells by pyroxamide may contribute to the antitumor effects of this agent[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 125 mg/mL (471.15 mM)
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Keywords | HDAC1 | inhibit | Apoptosis | Histone deacetylases | leukemia | Pyroxamide | HDAC | Inhibitor |
Inhibitors Related | Stavudine | 5-Fluorouracil | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Tributyrin | Curcumin |
Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Chromatin Modification Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |