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Rac-Belinostat

Catalog No. T1852   CAS 414864-00-9
Synonyms: NSC726630, PXD101, PX-105684

Rac-Belinostat (PX-105684) is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.

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Rac-Belinostat Chemical Structure
Rac-Belinostat, CAS 414864-00-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 62.00
25 mg In stock $ 98.00
50 mg In stock $ 147.00
100 mg In stock $ 217.00
200 mg In stock $ 347.00
500 mg In stock $ 578.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.96%
Purity: 99.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rac-Belinostat (PX-105684) is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.
Targets&IC50 HDAC:27 nM
Kinase Assay Histone Deacetylase Activity: Subconfluent cultures are harvested and washed twice in ice cold PBS and pelleted by centrifugation at 200 × g for 5 min. The cell pellet is resuspended in two volumes of lysis buffer [60 mM Tris buffer (pH 7.4) containing 30% glycerol and 450 mM NaCl] and lysed by three freeze (dry ice) thaw (30 °C water bath) cycles. Cell debris is removed by centrifugation at 1.2 × 104 g for 5 min, and the supernatant is stored at ?80 °C. Histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRK corresponding to the 20 NH2-terminal residues) is acetylated by a recombinant protein containing the hypoxanthine-aminopterin-thymidine domain of p300, using [3H]acetyl CoA as a source of acetate. H4 peptide (100 μg) is mixed with hypoxanthine-aminopterin-thymidine buffer (50 mM Tris HCl pH 8.0, 5% glycerol, 50 mM KCl, and 0.1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoethyl) benzenesulfonylfluoride, 1 × complete protease inhibitors, 50 μL of purified p300, and 1.85 m [3H]acetyl CoA (4.50Ci/mmol) in a final volume of 300 μL and incubated at 30 °C for 45 min. The p300 protein is removed by incubation with 20 μL of 50% Ni-agaroase beads for 1 hour at 4 °C and centrifugation. The supernatant is applied to a 2 mL Sephadex G15 column, and the flow through is collected. One milliliter of distilled Water is gently applied, and three drop fractions are collected; this is repeated until 4–5 mL of distilled Water has been added, and ~40 fractions are collected. Three microliters of each fraction are diluted in 2 mL of scintillation fluid and counted in a scintillation counter to identify the fractions containing the labeled peptide. These fractions are pooled, and 1 μL of the combined sample is measured to assess the radioactivity in every peptide batch (3-7×103 cpm/μL). For activity assays, the reaction is carried out in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] containing 2 μL of cell extract and, where used, 2 μL of belinostat.The reaction is started by the addition of 2 μL of [3H] labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples are incubated at 37 °C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12 M final concentrations, respectively). Released [3H]acetate is extracted into 750 μL of ethyl acetate, and samples are centrifuged at 1.2× 104 g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted.
Cell Research Tumor cell lines are seeded in 5 mL of medium at a density of 8 × 104 cells/25 cm2 flask and incubated for 48 hours. Cells are exposed to Belinostat (0.016 to 10 μM) for 24 hours. The medium is removed, and 1 mL of trypsin/EDTA is added to each flask. Once the cells have detached, 1 mL of medium is added, the cells are resuspended, and those from the control untreated flask are counted. Cells are diluted and plated into 6-cm Petri dishes (three per flask) at a density of 0.5-2× 103 cells/dish depending on the cell line. Cells from the drug-treated flasks are diluted and plated as for the control flasks. Dishes are incubated for 10–15 days at 37 °C. Cells are washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 defined as the concentration of belinostat required to reduce the number of colonies to 50% of that of the control untreated cells.(Only for Reference)
Synonyms NSC726630, PXD101, PX-105684
Molecular Weight 318.35
Formula C15H14N2O4S
CAS No. 414864-00-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (188.5 mM)

TargetMolReferences and Literature

1. Plumb JA, et al. Mol Cancer Ther, 2003, 2(8), 721-728. 2. Buckley MT, et al. J Transl Med, 2007, 5:49. 3. Qian X, et al. Mol Cancer Ther, 2006, 5(8), 2086-2095. 4. Chowdhury S, et al. J Biol Chem, 2011, 286(35), 30937-30948. 5. Duan J, et al. Mol Cancer Ther, 2007, 6(1), 37-50. 6. Zuo Y, Xu H, Chen Z, et al. 17‑AAG synergizes with Belinostat to exhibit a negative effect on the proliferation and invasion of MDA‑MB‑231 breast cancer cells[J]. Oncology Reports. 2020, 43(6): 1928-1944.

TargetMolCitations

1. Zuo Y, Xu H, Chen Z, et al. 17‑AAG synergizes with Belinostat to exhibit a negative effect on the proliferation and invasion of MDA‑MB‑231 breast cancer cells. Oncology Reports. 2020, 43(6): 1928-1944. 2. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Approved Drug Library NF-κB Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Rac-Belinostat 414864-00-9 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC NSC 726630 NSC726630 NSC-726630 Belinostat PX 105684 PX105684 PXD101 PXD 101 PX-105684 PXD-101 inhibitor inhibit

 

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