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Nexturastat A

Catalog No. T1819   CAS 1403783-31-2

Nexturastat A is an effective and specific HDAC6 inhibitor (IC50: 5 nM). Its selectivity is <190-fold than other HDACs.

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Nexturastat A Chemical Structure
Nexturastat A, CAS 1403783-31-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 63.00
5 mg In stock $ 90.00
10 mg In stock $ 117.00
25 mg In stock $ 197.00
50 mg In stock $ 318.00
100 mg In stock $ 473.00
1 mL * 10 mM (in DMSO) In stock $ 71.00
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Purity: 99.57%
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Biological Description
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Description Nexturastat A is an effective and specific HDAC6 inhibitor (IC50: 5 nM). Its selectivity is >190-fold than other HDACs.
Targets&IC50 HDAC6:5 nM
In vivo Nexturastat A significantly inhibits the growth of B16 melanoma cells in mice, with a GI50 of 14.3 μM. In these cells, Nexturastat A dose-dependently increases the levels of acetylated α-tubulin without affecting the acetylation of histone H3 associated with abscesses.
Kinase Assay HDAC inhibition assays: HDAC inhibition assays are performed by Reaction Biology Corp. using isolated human, recombinant full2length HDAC1 and -6 from a baculovirus expression system in Sf9 cells. An acetylated fluorogenic peptide,RHKKAc, derived from residues 379-382 of p53 is used as substrate. The reaction buffer is made up of 50 mM Tris-HCl pH 8.0, 127 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA, and a final concentration of 1% DMSO. Compounds are delivered in DMSO and delivered to enzyme mixture with preincubation of 5-10 min followed by substrate addition and incubation for 2 h at 30°C. Trichostatin A and developer are added to quench the reaction and generate fluorescence, respectively. Dose-response curves are generated starting at 30 μM compound with three-fold serial dilutions to generate a 10-dose plot. IC50 values are then generated from the resulting plots, and the values expressed are the average of duplicate trials ± standard deviation.
Cell Research B16 murine melanoma cells are plated at 5000/well in 96 well flat bottom plates. The following day, media is changed to that containing various concentrations of HDACi or matched DMSO vehicle concentrations diluted in complete medium done in triplicate. Cells are incubated for 48 hours at 37&deg;C and 5% CO2. Density of viable, metabolically active cells is quantified using a standard MTS assay as per manufacturer&rsquo;s instructions. Briefly, 20&mu;L of reagent are added per well and incubated at 37&deg;C for 3 hours. Absorbances at 490 nM are measured spectrophotometrically with background subtraction at 690 nM. All values are then normalized and expressed as a percentage of medium control (100%). (Only for Reference)
Molecular Weight 341.4
Formula C19H23N3O3
CAS No. 1403783-31-2

Storage

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

Solubility Information

DMSO: 63 mg/mL (184.5 mM)

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

Ethanol: 2 mg/mL (5.85 mM)

TargetMolReferences and Literature

1. Bergman JA, et al. J Med Chem. 2012, 55(22), 9891-9899.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Highly Selective Inhibitor Library Cancer Cell Differentiation Compound Library HIF-1 Signaling Pathway Compound Library Anti-Aging Compound Library Anti-Pancreatic Cancer Compound Library NF-κB Signaling Compound Library Histone Modification Compound Library Bioactive Compound Library Immunology/Inflammation Compound Library

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HDAC8-IN-4 Bakkenolide A ACY-738 M344 BEBT-908 HDAC1/CDK7-IN-1 HDAC-IN-7 PB131

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Keywords

Nexturastat A 1403783-31-2 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC inhibit Histone deacetylases Inhibitor inhibitor

 

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