Nexturastat A
Based on 3 publication(s) in Google Scholar
Nexturastat A is a potent, selective HDAC6 inhibitor. Nexturastat A has inhibitory for HDAC6 with an IC50 of 5 nM. Nexturastat A can be used for the research of multiple myeloma (MM).
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- Pureza: 98.69%
- No. CAS: 1403783-31-2
- Fòrmula: C19H23N3O3
- Peso molecular:341.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Nexturastat A
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Actividad biológica
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HDAC6 5.02 nM (IC50) |
HDAC8 0.954 μM (IC50) |
HDAC1 3.02 μM (IC50) |
HDAC7 4.46 μM (IC50) |
HDAC11 5.14 μM (IC50) |
HDAC3 6.68 μM (IC50) |
HDAC9 6.72 μM (IC50) |
HDAC2 6.92 μM (IC50) |
HDAC10 7.57 μM (IC50) |
HDAC4 9.39 μM (IC50) |
HDAC5 11.7 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 697 | IC50 |
401 nM
Compound: Nexturastat
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Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
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[PMID: 31710483] |
| B16 | GI50 |
14.3 μM
Compound: 5g, Nexturastat A
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Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay
Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay
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[PMID: 23009203] |
| MCF7 | IC50 |
1.4 μM
Compound: Nexturastat A
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Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
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[PMID: 29317150] |
| MM1.S | IC50 |
1.76 μM
Compound: Nexturastat
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Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
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[PMID: 35119267] |
| MV4-11 | IC50 |
1.68 μM
Compound: Nexturastat
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Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
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[PMID: 34101461] |
| MV4-11 | IC50 |
1.68 μM
Compound: Nexturastat
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Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
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[PMID: 35119267] |
| Sf9 | IC50 |
0.005 μM
Compound: NextA
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Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
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[PMID: 31414801] |
| Sf9 | IC50 |
2.86 μM
Compound: NextA
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Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
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[PMID: 31414801] |
| Sf9 | IC50 |
25 nM
Compound: Nexturastat
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Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
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[PMID: 31710483] |
| Sf9 | IC50 |
3020 nM
Compound: 5g, Nexturastat A
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Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
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[PMID: 23009203] |
| Sf9 | IC50 |
5.02 nM
Compound: 5g, Nexturastat A
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Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
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[PMID: 23009203] |
Nexturastat A (5 g) has inhibitory for HDAC6 with IC50 values of 0.005 μM[1].
Nexturastat A (0-10 μM; 24 h) has substrate selectivity for HDAC62[1].
Nexturastat A has antiproliferative activity against B16 murine melanoma cells with IC50 values of 14.3 μM[1].
Nexturastat A (NexA) (0-40 μM; 48 h) suppresses viability and induced G1 phase arrest of human MM cells[2].
Nexturastat A (0, 30, 40 μM; 48 h) promotes apoptosis of MM cells via transcriptional activation of the p21 promoter[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B16 murine melanoma cells
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Concentration:0-10 μM
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Incubation Time:24 h
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Result:Increased the level of acetyl α-tubulin levels in a dose-dependent.
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Cell Line:RPMI-8226 and U266 cells
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Concentration:0-40 µM
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Incubation Time:48 h
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Result:Impaired multiple myeloma (MM) cells viability in a dose- and time-dependent manner.
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Cell Line:RPMI-8226 and U266 cells
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Concentration:0, 30, 40 μM
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Incubation Time:48 h
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Result:Induced cell apoptosis in human MM cells.
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Cell Line:RPMI-8226 and U266 cells
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Concentration:30 µM
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Incubation Time:48 h
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Result:Increased the levels of p21 mRNA in RPMI-8226 and U266 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1403783-31-2
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Appearance Solid
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Peso molecular 341.40
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Fòrmula C19H23N3O3
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Color White to off-white
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SMILES
O=C(NO)C1=CC=C(CN(CCCC)C(NC2=CC=CC=C2)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Global crotonylome reveals hypoxia-mediated lamin A crotonylation regulated by HDAC6 in liver cancer. [Abstract]2022 Aug 17;13(8):717. PMID: 35977926 -
Mol Immunol
2023 Dec:164:98-111. PMID: 37992541 -
Solvente y solubilidad
DMSO : ≥ 56 mg/mL (164.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bergman JA, et al. Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J Med Chem. 2012 Nov 26;55(22):9891-9. [Content Brief]
[2]. Xiaoyang Sun, et al. The selective HDAC6 inhibitor Nexturastat A induces apoptosis, overcomes drug resistance and inhibits tumor growth in multiple myeloma. Biosci Rep. 2019 Mar 22;39(3):BSR20181916. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9291 mL | 14.6456 mL | 29.2912 mL | 73.2279 mL |
| 5 mM | 0.5858 mL | 2.9291 mL | 5.8582 mL | 14.6456 mL | |
| 10 mM | 0.2929 mL | 1.4646 mL | 2.9291 mL | 7.3228 mL | |
| 15 mM | 0.1953 mL | 0.9764 mL | 1.9527 mL | 4.8819 mL | |
| 20 mM | 0.1465 mL | 0.7323 mL | 1.4646 mL | 3.6614 mL | |
| 25 mM | 0.1172 mL | 0.5858 mL | 1.1716 mL | 2.9291 mL | |
| 30 mM | 0.0976 mL | 0.4882 mL | 0.9764 mL | 2.4409 mL | |
| 40 mM | 0.0732 mL | 0.3661 mL | 0.7323 mL | 1.8307 mL | |
| 50 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL | 1.4646 mL | |
| 60 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2205 mL | |
| 80 mM | 0.0366 mL | 0.1831 mL | 0.3661 mL | 0.9153 mL | |
| 100 mM | 0.0293 mL | 0.1465 mL | 0.2929 mL | 0.7323 mL |
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