Nexturastat A

Catalog No.S7473

For research use only.

Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.

Nexturastat A Chemical Structure

CAS No. 1403783-31-2

Selleck's Nexturastat A has been cited by 12 Publications

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Biological Activity

Description Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
Features Urea-based HDAC6-selective inhibitor.
Targets
HDAC6 [1]
(Cell-free assay)
5 nM
In vitro

In B16 murine melanoma cells, Nexturastat A leads to a dose-dependent increase of acetyl α-tubulin levels without a concomitant elevation of histone H3 acetylation. Moreover, Nexturastat A potently inhibits the growth of B16 melanoma cells with GI50 of 14.3 μM. [1]

Protocol (from reference)

Kinase Assay:

[1]

  • 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:

[1]

  • Cell lines: B16 murine melanoma cells
  • Concentrations: ~100 μM
  • Incubation Time: 48 hours
  • Method:

    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°C and 5% CO2. Density of viable, metabolically active cells is quantified using a standard MTS assay as per manufacturer’s instructions. Briefly, 20μL of reagent are added per well and incubated at 37°C for 3 hours. Absorbances at 490nM are measured spectrophotometrically with background subtraction at 690 nM. All values are then normalized and expressed as a percentage of medium control (100%).

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 341.4
Formula

C19 H23 N3 O3

CAS No. 1403783-31-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCN(CC1=CC=C(C=C1)C(=O)NO)C(=O)NC2=CC=CC=C2

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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