Size : 10mg
Phone : +1 850 650 7790
Synonyms:
| Description | Nexturastat A is an effective and specific HDAC6 inhibitor (IC50: 5 nM). Its selectivity is >190-fold than other HDACs. |
| Targets & IC50 | HDAC4:9.39 μM, HDAC1:3.02 μM, HDAC9:6.72 μM, HDAC7:4.46 μM, HDAC2:6.92 μM, HDAC5:11.7 μM, HDAC3:6.68 μM, HDAC11:5.14 μM, HDAC10:7.57 μM, HDAC6:5 nM, HDAC8:0.954 μM |
| 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°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 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 |
| Smiles | C(N(C(NC1=CC=CC=C1)=O)CCCC)C2=CC=C(C(NO)=O)C=C2 |
| Relative Density. | 1.228 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 63 mg/mL (184.53 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 2 mg/mL (5.86 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.86 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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