2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. Droxinostat

Droxinostat  (Synonyms: NS 41080)

Cat. No.: HY-13267 Purity: 98.91%
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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).

For research use only. We do not sell to patients.

Droxinostat Chemical Structure

Droxinostat Chemical Structure

CAS No. : 99873-43-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
1 mg USD 25 In-stock
5 mg USD 50 In-stock
10 mg USD 80 In-stock
25 mg USD 170 In-stock
50 mg USD 270 In-stock
100 mg USD 430 In-stock
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Based on 2 publication(s) in Google Scholar

Droxinostat Related Antibodies

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View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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)[1][2].

IC50 & Target[2]

HDAC8

1.46 μM (IC50)

HDAC6

2.47 μM (IC50)

HDAC3

16.9 μM (IC50)

In Vitro

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.

Droxinostat Related Antibodies

Western Blot Analysis[2]

Cell Line: SMMC-7721 and HepG2 (Human liver carcinoma cell lines)
Concentration: 0, 10, 20, or 40 μM
Incubation Time: 48 h
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.

Cell Proliferation Assay[2]

Cell Line: SMMC-7721 and HepG2
Concentration: 0, 10, 20, 40, and 80 μM
Incubation Time: 0, 24, 48, 72, 96, and 120 h
Result: Decreased the viability with a time-and dose-dependent in both cell lines.

Apoptosis Analysis[2]

Cell Line: SMMC-7721 and HepG2
Concentration: 0 to 80 μM
Incubation Time: 48 h
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.

RT-PCR[2]

Cell Line: SMMC-7721 and HepG2
Concentration: 20 μM and 40 μM
Incubation Time: 48 h
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.
Molecular Weight

243.69

Formula

C11H14ClNO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C(C)=C1)OCCCC(NO)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1036 mL 20.5179 mL 41.0357 mL
5 mM 0.8207 mL 4.1036 mL 8.2071 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 98.91%

COA (243 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

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
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Droxinostat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Droxinostat99873-43-5NS 41080NS41080NS-41080HDACApoptosisHistone deacetylaseshistone deacetylase (HDAC)HDAC3HDAC6HDAC8hepatocellular carcinoma (HCC)cancerInhibitorinhibitorinhibit

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