For research use only. Not for therapeutic Use.
Pyroxamide（Cat No.:R039814）is a histone deacetylase (HDAC) inhibitor with potential anti-cancer properties. By inhibiting HDACs, Pyroxamide promotes hyperacetylation of histones, leading to an open chromatin structure that reactivates the expression of tumor suppressor genes. This results in the inhibition of cancer cell proliferation, induction of differentiation, and apoptosis. Pyroxamide has shown promise in preclinical studies for various cancers, including solid tumors and hematologic malignancies. Its ability to modulate gene expression through epigenetic mechanisms makes it a valuable compound in the development of targeted cancer therapies, particularly in combination with other treatments.
| Catalog Number | R039814 |
| CAS Number | 382180-17-8 |
| Synonyms | N1-hydroxy-N8-3-pyridinyloctanediamide; N-hydroxy-N’-3-pyridinyloctanediamide; |
| Molecular Formula | C13H19N3O3 |
| Purity | ≥95% |
| Target | HDAC |
| Solubility | Soluble in DMSO > 10 mM |
| Storage | Store at -20°C |
| IUPAC Name | N'-hydroxy-N-pyridin-3-yloctanediamide |
| InChI | InChI=1S/C13H19N3O3/c17-12(15-11-6-5-9-14-10-11)7-3-1-2-4-8-13(18)16-19/h5-6,9-10,19H,1-4,7-8H2,(H,15,17)(H,16,18) |
| InChIKey | PTJGLFIIZFVFJV-UHFFFAOYSA-N |
| SMILES | C1=CC(=CN=C1)NC(=O)CCCCCCC(=O)NO |
| Reference | 1:Clin Cancer Res. 2001 Apr;7(4):962-70. Inhibition of transformed cell growth and induction of cellular differentiation by pyroxamide, an inhibitor of histone deacetylase.Butler LM,Webb Y,Agus DB,Higgins B,Tolentino TR,Kutko MC,LaQuaglia MP,Drobnjak M,Cordon-Cardo C,Scher HI,Breslow R,Richon VM,Rifkind RA,Marks PA, PMID: 11309347 </br><span>Abstract:</span> PURPOSE: We have synthesized a series of hybrid polar compounds that induce differentiation and/or apoptosis of various transformed cells. These agents are also potent inhibitors of histone deacetylases (HDACs). Pyroxamide (suberoyl-3-aminopyridineamide hydroxamic acid) is a new member of this class of compounds that is currently under development as an anticancer agent. We investigated the activity of pyroxamide as an inducer of differentiation and/or apoptosis in transformed cells.EXPERIMENTAL DESIGN AND RESULTS: Pyroxamide, at micromolar concentrations, induced terminal differentiation in murine erythroleukemia (MEL) cells and caused growth inhibition by cell cycle arrest and/or apoptosis in MEL, prostate carcinoma, bladder carcinoma, and neuroblastoma cells. Administration of pyroxamide (100 or 200 mg/kg/day) to nude mice at doses that caused little evident toxicity significantly suppressed the growth of s.c. CWR22 prostate cancer xenografts. Despite the potent growth-inhibitory effects of pyroxamide in this tumor model, serum prostate-specific antigen levels in control versus pyroxamide-treated mice were not significantly different. Pyroxamide is a potent inhibitor of affinity-purified HDAC1 (ID(50) = 100 nM) and causes the accumulation of acetylated core histones in MEL cells cultured with the agent. Human CWR22 prostate tumor xenografts from mice treated with pyroxamide (100 or 200 mg/kg/day) showed increased levels of histone acetylation and increased expression of the cell cycle regulator p21/WAF1, compared with tumors from vehicle-treated control animals.CONCLUSIONS: The findings suggest that 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. |
