Pyroxamide

SKU: orb1299613

Description

Pyroxamide is a potent small molecule inhibitor of histone deacetylases (HDACs), particularly HDAC1 (IC50: 0.1-0.2 µM), exhibiting antineoplastic activity. It is widely used in cancer research to study epigenetic mechanisms, demonstrating effects in both cellular assays and in vivo tumor models.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 382180-17-8
• MW: 265.31
• Purity: 98.77% (May vary between batches)
• Formula: C₁₃H₁₉N₃O₃
• SMILES: ONC(=O)CCCCCCC(=O)Nc1cccnc1
• Target: Apoptosis,HDAC
• Solubility: DMSO:125 mg/mL (471.15 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (15.08 mM)

Bioactivity

• Target IC50:
  HDAC1:0.1-0.2 μM
• 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.
• 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
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, HDAC1, HDAC, Histone deacetylases, leukemia, inhibit, Pyroxamide, Apoptosis

Compound Identifiers

PubChem CID

4996