Droxinostat
Based on 4 publication(s) in Google Scholar
Droxinostat (NS 41080) is a histone deacetylase (HDAC) inhibitor. Droxinostat selectively inhibits HDAC3, HDAC6, and HDAC8 with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively. Droxinostat can be used for the research of hepatocellular carcinoma (HCC).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.08%
- No. CAS: 99873-43-5
- Fòrmula: C11H14ClNO3
- Peso molecular:243.69
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Droxinostat
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Actividad biológica
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HDAC8 1.46 μM (IC50) |
HDAC6 2.47 μM (IC50) |
HDAC3 16.9 μM (IC50) |
Droxinostat selectively inhibits HDAC3, HDAC6, and HDAC8 with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively[1].
Droxinostat (0, 10, 20, or 40 μM; 48 h) suppresses HDAC3 expression and induces acetylation of histones H3 and H4[2].
Droxinostat (0, 10, 20, 40, and 80 μM; 0, 24, 48, 72, 96, and 120 h) inhibits cell proliferation and colony formation in HepG2 and SMMC-7721 cells[2].
Droxinostat (0 to 80 μM; 48 h) induces hepatoma cell apoptosis by activating mitochondrial apoptotic pathways and downregulating FLIP[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SMMC-7721 and HepG2 (Human liver carcinoma cell lines)
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Concentration:0, 10, 20, or 40 μM
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Incubation Time:48 h
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Result:Significantly decreased the expression of HDAC3 with dose-dependent in HepG2 and SMMC-7721 cell lines.
Significantly enhanced the expression of acetyl-H3 (Ac-H3) and acetylH4 (Ac-H4) in HepG2 and SMMC-7721 cells in a dose-dependent manner.
Upregulated the levels of phospho-p53 and cleaved caspase 3 protein and downregulated the levels of Bcl-2.
Markedly increased the Bax/Bcl-2 ratio in a dose-dependent manner and increased the expression of cleaved PARP protein in HepG2 cells in a dose-dependent manner.
Significant reduced the FLIP expression and enhanced caspase 8 activity in both HepG2 and SMMC-7721cell.
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Cell Line:SMMC-7721 and HepG2
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Concentration:0, 10, 20, 40, and 80 μM
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Incubation Time:0, 24, 48, 72, 96, and 120 h
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Result:Decreased the viability with a time-and dose-dependent in both cell lines.
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Cell Line:SMMC-7721 and HepG2
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Concentration:0 to 80 μM
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Incubation Time:48 h
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Result:Clearly led to dose-dependent apoptosis, but did not induce hepatoma cell apoptosis at 10 μM and had an apoptotic effect at a starting concentration of 20 μM.
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Cell Line:SMMC-7721 and HepG2
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Concentration:20 μM and 40 μM
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Incubation Time:48 h
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Result:Significantly increased the mRNA levels of Bax and p53 genes associated with the mitochondrial p53 apoptosis pathway in a dose-dependent manner in HepG2 and SMMC-7721 cells.
Significantly increased the Bcl-2 mRNA levels in SMMC-7721 cells at a concentration of 40 uM and also increased the Bax/Bcl-2 mRNA ratio.
Chemical Information
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No. CAS 99873-43-5
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Appearance Solid
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Peso molecular 243.69
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Fòrmula C11H14ClNO3
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Color White to off-white
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SMILES
ClC1=CC=C(C(C)=C1)OCCCC(NO)=O
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Synonyms
NS 41080
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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 (4)
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Journal Impact Factor
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Most Recent
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Cancer Res
Targeting the SP/KLF Transcriptional Regulatory Network Synergizes with HDAC Inhibition to Impede Progression of H3K27M Diffuse Intrinsic Pontine Glioma. [Abstract]2025 Jun 2;85(11):2100-2116. PMID: 40053472 -
Int J Mol Sci
Butyrate Prevents Induction of CXCL10 and Non-Canonical IRF9 Expression by Activated Human Intestinal Epithelial Cells via HDAC Inhibition. [Abstract]2022 Apr 2;23(7):3980. PMID: 35409339 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Solvente y solubilidad
DMSO : ≥ 150 mg/mL (615.54 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 (10.26 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 (10.26 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 (276 KB)
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SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Korean - KR (476 KB)
- Portuguese - PT (476 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liu J, et al. Droxinostat, a Histone Deacetylase Inhibitor, Induces Apoptosis in Hepatocellular Carcinoma Cell Lines via Activation of the Mitochondrial Pathway and Downregulation of FLIP. Transl Oncol. 2016 Feb;9(1):70-8. [Content Brief]
[2]. Wood TE et al. Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther. 2010 Jan;9(1):246-56. [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 | 4.1036 mL | 20.5179 mL | 41.0357 mL | 102.5894 mL |
| 5 mM | 0.8207 mL | 4.1036 mL | 8.2071 mL | 20.5179 mL | |
| 10 mM | 0.4104 mL | 2.0518 mL | 4.1036 mL | 10.2589 mL | |
| 15 mM | 0.2736 mL | 1.3679 mL | 2.7357 mL | 6.8393 mL | |
| 20 mM | 0.2052 mL | 1.0259 mL | 2.0518 mL | 5.1295 mL | |
| 25 mM | 0.1641 mL | 0.8207 mL | 1.6414 mL | 4.1036 mL | |
| 30 mM | 0.1368 mL | 0.6839 mL | 1.3679 mL | 3.4196 mL | |
| 40 mM | 0.1026 mL | 0.5129 mL | 1.0259 mL | 2.5647 mL | |
| 50 mM | 0.0821 mL | 0.4104 mL | 0.8207 mL | 2.0518 mL | |
| 60 mM | 0.0684 mL | 0.3420 mL | 0.6839 mL | 1.7098 mL | |
| 80 mM | 0.0513 mL | 0.2565 mL | 0.5129 mL | 1.2824 mL | |
| 100 mM | 0.0410 mL | 0.2052 mL | 0.4104 mL | 1.0259 mL |
Droxinostat Related Classifications
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