Molecular Weight(MW): 341.4
Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
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Cells were exposed to HDAC Class II selective inhibitors LMK-235 or Nexturastat A (NA) at the indicated concentrations for 48 hrs and analyzed by Western blotting. Rom, romidepsin; Bel, belinostat, Pano, panobinostat; SAHA, suberoylanilide hydroxamic acid.
Oncotarget, 2016, 7(39):63829-63838. Nexturastat A purchased from Selleck.
HDAC inhibitors disrupt SS18-SSX/TLE1 co-localization. A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells A, B. is also confirmed by immunoprecipitation C. The decrease in PLA co-localization signal correlates with apoptosis induction by HDAC inhibitor FK228 in SYO-1 cells.
Oncotarget, 2016. . Nexturastat A purchased from Selleck.
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Choose Selective HDAC Inhibitors
|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.|
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. 
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.
|In vitro||DMSO||68 mg/mL (199.17 mM)|
|Ethanol||2 mg/mL (5.85 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
C19 H23 N3 O3
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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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.
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