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Dacinostat

Catalog No. T2454   CAS 404951-53-7
Synonyms: NVP-LAQ824, LAQ824

LAQ824 (Dacinostat (NVP-LAQ824)) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.

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Dacinostat Chemical Structure
Dacinostat, CAS 404951-53-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 45.00
2 mg In stock $ 62.00
5 mg In stock $ 112.00
10 mg In stock $ 189.00
25 mg In stock $ 339.00
50 mg In stock $ 513.00
100 mg In stock $ 743.00
500 mg In stock $ 1,520.00
1 mL * 10 mM (in DMSO) In stock $ 112.00
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Purity: 95.28%
Purity: 95.28%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LAQ824 (Dacinostat (NVP-LAQ824)) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.
Targets&IC50 HDAC:32 nM
Kinase Assay In Vitro Histone Deacetylase Assay: HDAC enzymes are partially purified from H1299 cell lysate by ion exchange chromatography using the Q Sepharose Fast Flow column. Enzyme complexes are collected from 500 mg of total cell lysate by immunoprecipitation with cdk2 polyclonal antibody or cdk1/cdc2 monoclonal antibody. Immunoprecipitates are resuspended in kinase buffer (50 mM Hepes, pH 8, 10 mM MgCl2, 2.5 mM EDTA, 1 mM dithiothreitol, 20 mM ATP, 10 mM β-glycerophosphate, 0.1 mM NaVO4, 1 mM sodium fluoride, 50 mM ATP, 10 μCi of [γ-32P]ATP) along with 1 μg of pRb recombinant protein substrate (cdk2) or 10 mL of H1 histone mixture containing 20 μg of substrate (cdc2). Phosphorylated Rb and H1 histone are resolved by electrophoresis and quantitated using a PhosphorImager.
Cell Research Cell proliferation is measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay). The cells are seeded in 12-well dishes and cultured in RPMI 1640 containing 10% FBS. The cells are cultured in the presence of various concentrations of TSA (up to 1,000 ng/mL). To examine the growth inhibition by TSA, viable cell numbers are determined by trypan blue dye exclusion, counted in a Nesbauer-type hemocytometer for 0 hour, 24 hours, and 48 hours. The same amount of ethanol is added to the RPMI 1640 medium as the control experiment. All experiments are performed in duplicate and repeated 3 times The average background value (treatment with medium alone) is subtracted from each experimental well; triplicate values are averaged for each compound dilution. The following formulas are used to calculate the percentage of growth: If X<T0, %Growth=(X-T0)/T0*100; If X>T0, %Growth=(X-T0)/(GC-T0)*100. where T0 is the average value of T0 ? background, GC is the average value of untreated cells (in triplicate) ? background, and X is the average value of compound-treated cells (in triplicate)-background. The "% Growth" is plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.(Only for Reference)
Synonyms NVP-LAQ824, LAQ824
Molecular Weight 379.45
Formula C22H25N3O3
CAS No. 404951-53-7

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: 71 mg/mL (187.1 mM)

TargetMolReferences and Literature

1. Atadja P, et al. Cancer Res, 2004, 64(2), 689-695. 2. Wang H, et al. J Immuno, 2011, 186(7), 31986-31996.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library DNA Damage & Repair Compound Library ReFRAME Related Library Bioactive Compound Library Inhibitor Library Clinical Compound Library Human Metabolite Library Drug Repurposing Compound Library

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Keywords

Dacinostat 404951-53-7 Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair HDAC LAQ 824 LAQ-824 NVP-LAQ824 NVP-LAQ 824 NVP-LAQ-824 Histone deacetylases inhibit Inhibitor LAQ824 inhibitor

 

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