Home Epigenetics HDAC inhibitor Pyroxamide (NSC 696085) For research use only.

Pyroxamide (NSC 696085)

Synonyms: NSC-696085

Pyroxamide(NSC 696085) is a potent inhibitor of affinity-purified HDAC1 with ID50 of 100 nM. It also induces growth suppression and cell death in human rhabdomyosarcoma in vitro.

Pyroxamide (NSC 696085) Chemical Structure

Pyroxamide (NSC 696085) Chemical Structure

CAS: 382180-17-8

Purity & Quality Control

Batch: S219001 DMSO] 17 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 98.99%
98.99

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Biological Activity

Description Pyroxamide(NSC 696085) is a potent inhibitor of affinity-purified HDAC1 with ID50 of 100 nM. It also induces growth suppression and cell death in human rhabdomyosarcoma in vitro.
In vitro
In vitro

Pyroxamide causes the accumulation of acetylated core histones in MEL cells cultured with the agent. Pyroxamide, at micromolar concentrations, induces terminal differentiation and inhibits proliferation of murine erythroleukemia(MEL) cells. Pyroxamide (1.25-20 mM) causes dose-dependent inhibition of growth by cell cycle arrest of prostate carcinoma (LNCaP), neuroblastoma (KCN-69n), and bladder carcinoma (T24) cells in culture, with similar efficacy in all of the cell lines. [1] A concentration of 1.25-20.0 μM Pyroxamide causes a dose-dependent decrease in viable cell number and an increase in percentage of dead cells over time in two Rhabdomyosarcoma cell lines, RD (embryonal ) and RH30B (alveolar). Accumulation of acetylated histones and induction of p21/WAF1 expression are obersevd in cells exposed to Pyroxamide. [2] Pyroxamide shows a dose- and time-dependent proliferation inhibition, induction of apoptosis and histone H4 hyperacetylation in three B-cell precursor (BCP)-acute lymphoblastic leukemia (ALL) cell lines (Reh, Nalm6, Z33). The calculated IC50 after 96 hours of Pyroxamide incubation are 2-6 μM. [3]
Kinase Assay HDAC Inhibition Assays
A MEL cell line expressing the epitope Flag-tagged HDAC1 is generated. HDAC1-Flag is affinity purified by immune-precipitation using M2 anti-Flag antibody-coated agarose, followed by elution from the agarose using the Flag peptide. [3H]acetate-labeled cellular histones are prepared from MEL cells and are used as a substrate for the HDAC activity assay. Released [3H] acetic acid is quantified by scintillation counting. For inhibition studies, the enzyme preparations are preincubated with Pyroxamide (10 to 100,000 nM) for 30 minutes at 4 °
Cell Research Cell lines MEL Ds19/Sc9 cells
Concentrations 0.625-8 μM
Incubation Time 5 days
Method

1-2 × 105 cells/mL MEL Ds19/Sc9 cells are cultured with increasing concentrations of Pyroxamide (0.625-8 μM) for 5 days, at which time the Benzidine positivity is determined as an indicator of terminal differentiation. MEL cell density is measured using a Coulter counter and viability is assessed by trypan blue exclusion.
In Vivo
In vivo

Administration of 100 or 200 mg/kg of Pyroxamide daily for 21 days causes significant, dose-dependent suppression of the growth of the tumor xenograft. A dose of 300 mg/kg Pyroxamide is lethal to all of the mice in the treatment group within 1 week. After in vivo administration of Pyroxamide, accumulation of acetylated histones and a dose-dependent increase in the expression of p21/WAF1 protein level are observed. [1]
Animal Research Animal Models Human CWR22 prostate cancer xenograft is s.c. injected in nude mice.
Dosages 100, 200, or 300 mg/kg
Administration Administered daily via i.p. injection.

Chemical Information & Solubility

Molecular Weight 265.31 Formula

C13H19N3O3
CAS No. 382180-17-8 SDF Download Pyroxamide (NSC 696085) SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 17 mg/mL ( (64.07 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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