Pyroxamide 是一种组蛋白脱乙酰基酶 1 抑制剂，ID50为 100 nM。 它可以诱导白血病细胞凋亡和细胞周期停滞。

Pyroxamide is an histone deacetylases (HDACs) inhibitor with antineoplastic properties ( HDAC1;IC50: 0.1-0.2 μM).

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]

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].

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]

382180-17-8

C13H19N3O3

265.313

DMSO:125 mg/mL (471.15 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years