1. Apoptosis Anti-infection Membrane Transporter/Ion Channel Neuronal Signaling
  2. Bcl-2 Family Caspase Apoptosis HSV Na+/K+ ATPase Calcium Channel
  3. Digitoxin

Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .

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

Digitoxin Chemical Structure

Digitoxin Chemical Structure

CAS No. : 71-63-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 67 In-stock
Solution
10 mM * 1 mL in DMSO USD 67 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 80 In-stock
50 mg USD 240 In-stock
100 mg USD 360 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Digitoxin:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure [1][2][3][4][5].

IC50 & Target

Bcl-2

 

Caspase-9

 

Caspase 3

 

Bax

 

HSV-1

 

In Vitro

Digitoxin (0-80 nM, 72 h) compromised cell survival in PC12 cells[1].
Digitoxin (4-1000 nM, 24-48 h) has an antitumor effects in MHCC97H, A549, HCT116 and HeLa cells[3].
Digitoxin (4-100 nM, 24-48 h) disrupts the cell cycle in HeLa cells[3].
Digitoxin (20-500 nM, 48 h) activates mitochondrial apoptosis in HeLa cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: MHCC97H, A549, HCT116 and HeLa cells
Concentration: 4-1000 nM
Incubation Time: 24 h, 48 h
Result: Dcreased the viability of these cancer cells in a dose- and time-dependent manner, with the IC50 values ranging from 0.075 to 0.395 µM following digitoxin treatment for 24 h and from 0.028 to 0.077 µM following digitoxin treatment for 48 h.

Cell Cycle Analysis[3]

Cell Line: HeLa cells
Concentration: 4 nM, 20 nM, 100 nM
Incubation Time: 24 h, 36 h, 48 h
Result: Increased cell population in the G2/M phase from 16.27 to 18.36, 23.46 and 31.51% at concentrations of 20 nM for12, 24 and 36 h.
Increased average cell population in the G2/M phase from 16.27 to 28.07% at concentrations of 4, 20 and 100 nM for 24 h.
Significantly decreased the protein expression levels of total CDK1 and phosphorylated CDK1.

Apoptosis Analysis[3]

Cell Line: HeLa cells
Concentration: 20 nM, 100 nM, 500 nM
Incubation Time: 48 h
Result: Upregulated Bax expression and unaltered Bcl-2 expression.
Significantly increased the expression of cytochrome c.
In Vivo

Digitoxin (1-2 mg/kg, Intraperitoneal injection, once a day for 19 days) has anticancer effects in nude mice[3].
Digitoxin (0.3-3 μg/kg, Intraperitoneal injection, once a day for 4 days) blocks the host over-production of cytokines in the cotton rat lung[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: nude mice harboring HeLa tumor xenografts[3]
Dosage: 1 mg/kg, 2 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Decreased the tumor volume from 330.71±45.61 to 214.56.93±73.25 mm.
Strongly increased the protein levels of cleaved caspase-3.
Reduced the number of Ki-67-positive cells.
Animal Model: cotton rats[4]
Dosage: 0.3 μg/kg, 1 μg/kg, 3 μg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Blocked cytokine storm.
Differentially affected cytokine expression.
Left immune cell density intact in virus-infected lung.
Clinical Trial
Molecular Weight

764.94

Formula

C41H64O13

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1O[C@](O[C@@H]2[C@@H](C)O[C@](O[C@H]3[C@@H](O)C[C@@](O[C@@H]4C[C@](CC[C@]5([H])[C@]6([H])CC[C@@]7(C)[C@]5(O)CC[C@@H]7C(CO8)=CC8=O)([H])[C@]6(C)CC4)([H])O[C@@H]3C)([H])C[C@@H]2O)([H])C[C@H](O)[C@@H]1O

Structure Classification
Initial Source
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 : 100 mg/mL (130.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3073 mL 6.5365 mL 13.0729 mL
5 mM 0.2615 mL 1.3073 mL 2.6146 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (3.27 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 (3.27 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:

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(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: 99.36%

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 1.3073 mL 6.5365 mL 13.0729 mL 32.6823 mL
5 mM 0.2615 mL 1.3073 mL 2.6146 mL 6.5365 mL
10 mM 0.1307 mL 0.6536 mL 1.3073 mL 3.2682 mL
15 mM 0.0872 mL 0.4358 mL 0.8715 mL 2.1788 mL
20 mM 0.0654 mL 0.3268 mL 0.6536 mL 1.6341 mL
25 mM 0.0523 mL 0.2615 mL 0.5229 mL 1.3073 mL
30 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0894 mL
40 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8171 mL
50 mM 0.0261 mL 0.1307 mL 0.2615 mL 0.6536 mL
60 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.5447 mL
80 mM 0.0163 mL 0.0817 mL 0.1634 mL 0.4085 mL
100 mM 0.0131 mL 0.0654 mL 0.1307 mL 0.3268 mL
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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.

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