Home Epigenetics HDAC inhibitor Pyroxamide (NSC 696085)

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Pyroxamide (NSC 696085) HDAC inhibitor

Cat.No.S2190

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

Chemical Structure

Molecular Weight: 265.31

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 265.31 Formula

C13H19N3O3

 Storage (From the date of receipt)
CAS No. 382180-17-8 Download SDF Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 17 mg/mL (64.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
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Mechanism of Action

Targets/IC50/Ki
HDAC1 [1]
100 nM(ID50)
In vitro

Pyroxamide (NSC 696085) causes the accumulation of acetylated core histones in MEL cells cultured with the agent. At micromolar concentrations, it induces terminal differentiation and inhibits proliferation of murine erythroleukemia(MEL) cells. This compound (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 it. [2] It 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 its 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 (NSC 696085) (10 to 100,000 nM) for 30 minutes at 4 °
In vivo

Administration of 100 or 200 mg/kg of Pyroxamide (NSC 696085) daily for 21 days causes significant, dose-dependent suppression of the growth of the tumor xenograft. A dose of 300 mg/kg of this compound is lethal to all of the mice in the treatment group within 1 week. After in vivo administration, accumulation of acetylated histones and a dose-dependent increase in the expression of p21/WAF1 protein level are observed. [1]
References

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