2. Cell Cycle/DNA Damage Epigenetics Apoptosis Immunology/Inflammation TGF-beta/Smad PI3K/Akt/mTOR Stem Cell/Wnt
  3. HDAC TNF Receptor Interleukin Related TGF-β Receptor IFNAR PI3K PKC Akt GSK-3 Caspase Apoptosis
  4. Bakkenolide A

Bakkenolide A is an anticancer agent. Bakkenolide A reduces the viability of leukemia cells, inhibits cell colony formation and invasion, and downregulates the expression of HDAC3 in cells. Bakkenolide A downregulates the expression of pro-inflammatory cytokines including TNF-α, interleukins such as IL-1β, TGF-β1 and IFN-γ, as well as the expression of PI3K, PDK and PKC in leukemia cells. Bakkenolide A downregulates activated Akt, GSK and Bad, while upregulates Cyto-c, cleaved Caspase3 and cleaved Caspase7, induces apoptosis (apoptosis) in leukemia cells and thereby inhibits inflammatory responses in leukemia cells. Bakkenolide A significantly slows the growth of subcutaneous leukemia tumors in nude mice. Bakkenolide A is applicable to leukemia-related research.

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

Bakkenolide A

Bakkenolide A Chemical Structure

CAS No. : 19906-72-0

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Bakkenolide A Related Antibodies

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

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP GDF15

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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Akt Akt1 Akt2 Akt3

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GSK-3 GSK-3α GSK-3β

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Bakkenolide A is an anticancer agent. Bakkenolide A reduces the viability of leukemia cells, inhibits cell colony formation and invasion, and downregulates the expression of HDAC3 in cells. Bakkenolide A downregulates the expression of pro-inflammatory cytokines including TNF-α, interleukins such as IL-1β, TGF-β1 and IFN-γ, as well as the expression of PI3K, PDK and PKC in leukemia cells. Bakkenolide A downregulates activated Akt, GSK and Bad, while upregulates Cyto-c, cleaved Caspase3 and cleaved Caspase7, induces apoptosis (apoptosis) in leukemia cells and thereby inhibits inflammatory responses in leukemia cells. Bakkenolide A significantly slows the growth of subcutaneous leukemia tumors in nude mice. Bakkenolide A is applicable to leukemia-related research[1].

In Vitro

Bakkenolide A (50-250 μM; 8-80 h) reduces the viability of human leukemia K562 cells, inhibits cell colony formation and invasion, and downregulates the mRNA and protein expression of HDAC3 in cells[1].
Bakkenolide A (200 μM; 48 h) significantly downregulates the expression of proinflammatory cytokines TNF-α, IL-1β, IL-18, IL-6, IL-8, IL-2, TGF-β1, IFN-γ and IL-17, as well as the expression of PI3K, PDK and PKC, in human leukemia K562 cells[1].
Bakkenolide A (200 μM; 48 h) induces apoptosis in human leukemia K562 cells by downregulating activated Akt, GSK and Bad, while upregulating cytochrome c (Cyto-c), cleaved Caspase3 and cleaved Caspase7[1].

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

Bakkenolide A Related Antibodies

Cell Viability Assay[1]

Cell Line: human leukemia K562 cells
Concentration: 50, 100,
150, 200 and 250 mM (48 h viability assay); 200 μM (time-dependent viability assay)
Incubation Time: 48 h (50, 100, 150, 250 μM); 8, 16, 24, 32, 40, 48, 56, 64, 72 and 80 h (200 μM)
Result: Reduced K562 cell viability in a time-dependent manner at 200 μM, with significant inhibition observed at 48 h and later time points.
Reduced K562 cell viability at 50, 100, 150, 200, and 250 μM for 48 h, with the most stable and effective inhibition seen at 200 μM.

RT-PCR[1]

Cell Line: human leukemia K562 cells
Concentration: 200 μM
Incubation Time: 48 h
Result: Significantly reduced HDAC3 mRNA expression in K562 cells to levels similar to those seen in HDAC3-knockdown K562 cells.

Cell Invasion Assay[1]

Cell Line: human leukemia K562 cells
Concentration: 200 μM
Incubation Time: 48 h
Result: Significantly reduced the invasive capacity of K562 cells, with relative invasion rates reduced to levels similar to those seen in HDAC3-knockdown K562 cells.

Western Blot Analysis[1]

Cell Line: human leukemia K562 cells
Concentration: 200 μM
Incubation Time: 48 h
Result: Significantly reduced protein expression of TNF-α, IL-1β, and IL-18 in K562 cells.

Immunofluorescence[1]

Cell Line: human leukemia K562 cells
Concentration: 200 μM
Incubation Time: 48 h
Result: Significantly reduced PI3K expression in K562 cells.

Apoptosis Analysis[1]

Cell Line: human leukemia K562 cells
Concentration: 200 μM
Incubation Time: 48 h
Result: Significantly accelerated apoptosis in K562 cells via flow cytometry.
Reduced activated (phosphorylated) Akt, GSK, and Bad protein expression in K562 cells.
Increased Cyto-c, cleaved Caspase3, and cleaved Caspase7 protein expression in K562 cells.
In Vivo

Bakkenolide A (200 μM pre-treatment of K562 cells, s.c., single administration) significantly slows the growth of subcutaneous leukemia tumors in Balb/c nude mice, reduces the expression level of HDAC3 in tumor tissues, increases the level of Caspase3, and decreases the final tumor weight after mice are sacrificed[1].

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

Animal Model: Balb/c nude mice[1]
Dosage: 200 μM pre-treatment of K562 cells (5 x 106 per mouse)
Administration: s.c., single administration
Result: Significantly slowed the growth of subcutaneous leukemia tumors in Balb/c nude mice, reduced HDAC3 expression levels in tumor tissues, increased caspase3 levels, and decreased the final tumor weight of mice after sacrifice.
Molecular Weight

234.33

Formula

C15H22O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]12C[C@@]3([H])CCC[C@H](C)[C@@]3(C)C2)OCC1=C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (213.37 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 4.2675 mL 21.3374 mL 42.6749 mL
5 mM 0.8535 mL 4.2675 mL 8.5350 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 (protect from light). 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: ≥ 1.25 mg/mL (5.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (5.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.99%

SDS (252 KB)

COA (258 KB) RP-HPLC (234 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, 6 months; -20°C, 1 month (protect from light). 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 4.2675 mL 21.3374 mL 42.6749 mL 106.6871 mL
5 mM 0.8535 mL 4.2675 mL 8.5350 mL 21.3374 mL
10 mM 0.4267 mL 2.1337 mL 4.2675 mL 10.6687 mL
15 mM 0.2845 mL 1.4225 mL 2.8450 mL 7.1125 mL
20 mM 0.2134 mL 1.0669 mL 2.1337 mL 5.3344 mL
25 mM 0.1707 mL 0.8535 mL 1.7070 mL 4.2675 mL
30 mM 0.1422 mL 0.7112 mL 1.4225 mL 3.5562 mL
40 mM 0.1067 mL 0.5334 mL 1.0669 mL 2.6672 mL
50 mM 0.0853 mL 0.4267 mL 0.8535 mL 2.1337 mL
60 mM 0.0711 mL 0.3556 mL 0.7112 mL 1.7781 mL
80 mM 0.0533 mL 0.2667 mL 0.5334 mL 1.3336 mL
100 mM 0.0427 mL 0.2134 mL 0.4267 mL 1.0669 mL
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Bakkenolide A 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:

Bakkenolide A19906-72-0HDACTNF ReceptorInterleukin RelatedTGF-β ReceptorIFNARPI3KPKCAktGSK-3CaspaseApoptosisHistone deacetylasesTumor Necrosis Factor ReceptorTNFRILTransforming growth factor beta receptorsInterferon-α/β receptorInterferon-alpha/beta receptor Phosphoinositide 3-kinaseProtein kinase CPKBProtein kinase BGlycogen synthase kinase-3Glycogen synthase kinase 3anticancer agentK562 cellsBalb/c nude miceleukemiaInhibitorinhibitorinhibit

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