1. Apoptosis Cell Cycle/DNA Damage
  2. Apoptosis MDM-2/p53 Bcl-2 Family CDK
  3. Diosbulbin B

Diosbulbin B, a diterpene lactone, is an anticancer agent. Diosbulbin B is an orally active component of Dioscorea. bulbifera L. Diosbulbin B can inhibit cell proliferation, induce G0/G1 phase arrest and apoptosis. Diosbulbin B can induce autophagy and mitochondrial dysfunction. Diosbulbin B can induce liver injury. Diosbulbin B can be used for the research of cancer, such as non-small cell lung cancer (NSCLC).

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

Diosbulbin B

Diosbulbin B Chemical Structure

CAS No. : 20086-06-0

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Diosbulbin B

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Diosbulbin B, a diterpene lactone, is an anticancer agent. Diosbulbin B is an orally active component of Dioscorea. bulbifera L. Diosbulbin B can inhibit cell proliferation, induce G0/G1 phase arrest and apoptosis. Diosbulbin B can induce autophagy and mitochondrial dysfunction. Diosbulbin B can induce liver injury. Diosbulbin B can be used for the research of cancer, such as non-small cell lung cancer (NSCLC)[1][2][3].

In Vitro

Diosbulbin B (0.5-400 μM, 24-72 h) inhibits proliferation in A549 and PC-9 cells, with IC50 values of 44.61 and 22.78 μM, respectively[1].
Diosbulbin B (12.5-100 μM, 24 h) enhances the ratio of cells in the G0/G1 phase in A549 and PC-9 cells[1].
Diosbulbin B (12.5-100 μM, 48 h) induces apoptosis in A549 and PC-9 cells[1].
Diosbulbin B (12.5-100 μM, 48 h) inhibits colony formation in A549 and PC-9 cells[1].
Diosbulbin B (12.5-100 μM, 48 h) reduces the levels of YY1 and apoptosis-related proteins and increases p53 levels in A549 and PC-9 cells[1].
Diosbulbin B (50-200 μM, 48h) induces autophagy and apoptosis in L-02 hepatocytes[3].
Diosbulbin B (50-200 μM, 48 h) causes mitochondrial dysfunction in L-02 hepatocytes[3].

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

Cell Cycle Analysis[1]

Cell Line: A549 and PC-9 cells
Concentration: 12.5, 25, 50 and 100 μM
Incubation Time: 24 h
Result: Markedly enhanced the ratio of cells in the G0/G1 phase.
Decreased the proportion of cells in the S phase and G2/M phase.

Western Blot Analysis[1]

Cell Line: A549 and PC-9 cells
Concentration: 12.5, 25, 50 and 100 μM
Incubation Time: 48 h
Result: Reduced the level of YY1 protein and increased p53 levels.
Suppressed the expression of Cyclin A2 and B2, along with the CDK1, CDK2, CDK4 and BCL-2.

Western Blot Analysis[3]

Cell Line: L-02 hepatocytes
Concentration: 50, 100 and 200 μM
Incubation Time: 48 h
Result: Increased LC3 II/I and Beclin-1 levels and decreased P62 levels.
Enhanced protein expression of Bax and up-regulated activities of caspase-3 and caspase-9.
In Vivo

Diosbulbin B (5-15 mg/kg, i.p., daily for 2 weeks) inhibits tumor growth in xenograft A549 tumor mice models[1].
Diosbulbin B (16-64 mg/kg, i.g., daily for 12 days) induces liver injury in ICR mice[2].

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

Animal Model: Xenograft A549 tumor mice models[1]
Dosage: 5 and 15 mg/kg
Administration: Intraperitoneally injection, daily for 2 weeks
Result: Reduced tumor volume and weight.
Did not result in any alterations in both body weight and organ coefficient.
Induced tumor cells disorganized and underwent apoptosis.
Reduced the level of YY1 protein and increased p53 levels.
Suppressed the expression of Cyclin A2 and B2, along with the CDK1, CDK2, and CDK4.
Animal Model: ICR mice (male, 18-22 g)[2]
Dosage: 16, 32 and 64 mg/kg
Administration: Orally gavage, daily for 12 days
Result: Increased the values of ALT, AST, ALP and MDA.
Lost normal architecture inliver.
Reduced glutathione levels and GST, GPx, SOD and CAT activities.
Molecular Weight

344.36

Formula

C19H20O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1OC2([H])C3([H])[C@](CC4([H])OC(C3([H])C4)=O)([H])C5(C)C1(C2)O[C@@H](C6=COC=C6)C5

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16 mg/mL (46.46 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 2.9039 mL 14.5197 mL 29.0394 mL
5 mM 0.5808 mL 2.9039 mL 5.8079 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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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: ≥ 1.33 mg/mL (3.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.3 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: ≥ 1.33 mg/mL (3.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.3 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)

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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: 99.90%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9039 mL 14.5197 mL 29.0394 mL 72.5984 mL
5 mM 0.5808 mL 2.9039 mL 5.8079 mL 14.5197 mL
10 mM 0.2904 mL 1.4520 mL 2.9039 mL 7.2598 mL
15 mM 0.1936 mL 0.9680 mL 1.9360 mL 4.8399 mL
20 mM 0.1452 mL 0.7260 mL 1.4520 mL 3.6299 mL
25 mM 0.1162 mL 0.5808 mL 1.1616 mL 2.9039 mL
30 mM 0.0968 mL 0.4840 mL 0.9680 mL 2.4199 mL
40 mM 0.0726 mL 0.3630 mL 0.7260 mL 1.8150 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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