Nexturastat A

Catalog No.S7473

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

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Nexturastat A Chemical Structure

Nexturastat A Chemical Structure
Molecular Weight: 341.4

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Product Description

Biological Activity

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

Protocol(Only for Reference)

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 Assay:


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

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%).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


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

Chemical Information

Download Nexturastat A SDF
Molecular Weight (MW) 341.4

C19 H23 N3 O3

CAS No. 1403783-31-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 68 mg/mL (199.17 mM)
Ethanol 2 mg/mL (5.85 mM)
Water <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* 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.
Chemical Name Benzamide, 4-​[[butyl[(phenylamino​)​carbonyl]​amino]​methyl]​-​N-​hydroxy-

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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