2. Anti-infection NF-κB MAPK/ERK Pathway Metabolic Enzyme/Protease Apoptosis
  3. Parasite NF-κB p38 MAPK Phosphatase Apoptosis
  4. Bruceine A

Bruceine A  (Synonyms: Dihydrobrusatol; NSC310616)

Cat. No.: HY-N0841 Purity: 98.01%
SDS
COA
Handling Instructions Technical Support

Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research.

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

Bruceine A Chemical Structure

Bruceine A Chemical Structure

CAS No. : 25514-31-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Bruceine A Related Antibodies

Top Publications Citing Use of Products

View All Parasite Isoform Specific Products:

View All Isoforms
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research[1][2][3][4][5].

IC50 & Target[1]

PFKFB4

44 nM (Kd)

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.082 μM
Compound: 9b
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by WST-1 assay
[PMID: 33289552]
LNCaP ED50
96 nM
Compound: 7
Cytotoxicity against hormone-dependent human LNCAP cells after 2 days by sulforhodamine B assay
Cytotoxicity against hormone-dependent human LNCAP cells after 2 days by sulforhodamine B assay
[PMID: 19026551]
Lu1 ED50
79 nM
Compound: 7
Cytotoxicity against human Lu1 cells after 2 days by sulforhodamine B assay
Cytotoxicity against human Lu1 cells after 2 days by sulforhodamine B assay
[PMID: 19026551]
MCF7 IC50
0.18 μM
Compound: 9b
Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-7 cells incubated for 72 hrs by MTT assay
[PMID: 33289552]
MCF7 ED50
1.5 nM
Compound: 7
Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay in presence of 43 uM (-)-hydnocarpin
Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay in presence of 43 uM (-)-hydnocarpin
[PMID: 19026551]
MCF7 ED50
15 nM
Compound: 7
Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay
[PMID: 19026551]
MDA-MB-231 IC50
0.23 μM
Compound: 9b
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
[PMID: 33289552]
In Vitro

Bruceine A (6.25-100 nM/0.08-20 μM, 24-72 h) inhibits the viability of pancreatic cancer cell lines MIA PaCa-2, SW1990, PANC-1 and AsPC-1 cells in a time- and dose-dependent manner[1].
Bruceine A (12.5-50 nM, 24 h) increases the percentage of MIA PaCa-2 cells in the G1 phase[1].
Bruceine A (12.5-50 nM, 24 h) induces apoptosis of MIA PaCa-2 cells in a dose-dependent manner[1].
Bruceine A (12.5-50 nM, 24 h) inhibits the mRNA expression level of PFKFB4 in MIA PaCa-2 cells[1].
Bruceine A (30-120 nM/0.3-1.2 μM, 24-48 h) inhibits the viability of MDA-MB-231 (IC50: 78.4 nM) and 4T1 (IC50: 524.6 nM) cells in triple negative breast cancer (TNBC) cell lines[2].
Bruceine A (7.5-30 nM/150-450 nM, 48 h) causes G0-G1 cell cycle arrest in MDA-MB-231 and 4T1 cells[2].
Bruceine A (60-240 nM/0.6-2.4 μM, 48 h) induces apoptosis (58.37% and 56.21%) in MDA-MB-231 and 4T1 cells in a dose-dependent manner[2].
Bruceine A (30-120 nM/0.3-1.2 μM, 24 h) inhibits the migration of MDA-MB-231 and 4T1 cells in a concentration-dependent manner[2].
Bruceine A (72 h) inhibits the activity of Entamoeba histolytica (IC50: 222.0 nM), Plasmodium falciparum (IC50: 21.0 nM), Babesia gibbsii (IC50: 7.7 nM), and Trypanosoma evansi (IC50: 2.9 nM)[3].
Bruceine A (2 h) inhibits the activity of NF-κB in Hela cells (IC50: 5.3 μg/mL)[4].
Bruceine A activates the p38α MAPK signaling pathway in MIA PaCa-2 cells[5].

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

Bruceine A Related Antibodies

Cell Viability Assay[1]

Cell Line: MIA PaCa-2 cells; SW1990, PANC-1 and AsPC-1 cells
Concentration: 6.25, 12.5, 25, 50 and 100 nM; 0.08, 0.31, 1.25, 5 and 20 μM
Incubation Time: 24, 48 and 72 h
Result: Inhibited the growth of adenocarcinoma cell lines MIA PaCa-2, SW1990, PANC-1, and AsPC-1 cells.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 12.5, 25 and 50 nM
Incubation Time: 24 h
Result: Down-regulated protein levels of CDK4, CDK6 and Cyclin D1.
Increased the expression of apoptosis-related proteins cleaved caspase3, cleaved caspase9, and cleaved PARP.

RT-PCR[1]

Cell Line: MIA PaCa-2 cells
Concentration: 12.5, 25 and 50 nM
Incubation Time: 24 h
Result: Inhibited the mRNA expression level of PFKFB4 in MIA PaCa-2 cells.

Cell Viability Assay[2]

Cell Line: MDA-MB-231 and 4T1 cells
Concentration: 24 and 48 h
Incubation Time: 24, 48 and 72 h
Result: Inhibits the proliferation activity of MDA-MB-231 and 4T1 cells.

Western Blot Analysis[2]

Cell Line: MDA-MB-231 and 4T1 cells
Concentration: 30, 60 and 120 nM; 0.3, 0.6 and 1.2 μM
Incubation Time: 24 h
Result: Down-regulated the protein expression levels of CDK4, CDK6 and Cyclin D1.
Up-regulated the protein expression levels of Bax, Cyt C and Cleaved-Caspase-3/9.
Down-regulated the protein expression levels of Bcl-2, PARP and Caspase-3/9.
Down-regulated the protein expression levels of MMP2 and MMP9.
In Vivo

Bruceine A (0.02-0.5 mg/kg, i.v., once every day for 10 d) exhibits antitumor activity in mice with the BALB/c nude mouse pancreatic cancer model[1][4].
Bruceine A (2-4 mg/kg, i.p., once every day for 2 weeks) has antitumor activity in mice with 4T1 xenograft tumor model[2].
Bruceine A (2-4 mg/kg, i.p., once every day for 17 d) inhibits lung metastasis in mice with 4T1-luc breast cancer lung metastasis model[2].

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

Animal Model: BALB/c athymic male nude mice pancreatic cancer model (6 weeks old)[1]
Dosage: 0.02, 0.1, 0.5 mg/kg
Administration: Intravenous injection (i.v.), once every day for 10 d
Result: Inhibited tumor growth.
Reduced protein levels of PFKFB4 and GSK3β in tumor tissues.
Reduced PCNA and Ki67 positive cells.
Animal Model: 4T1 xenograft tumor model (female BALB/c mice, 6-8 weeks old, 18-20 g)[2]
Dosage: 2 and 4 mg/kg
Administration: Intraperitoneal injection (i.p.), once every day for 2 weeks
Result: Inhibited tumor growth.
Reduced Ki67 proliferation marker staining and p-MEK staining.
Animal Model: 4T1-luc breast cancer lung metastasis model (female BALB/c mice, 6-8 weeks old, 18-20 g)[2]
Dosage: 2 and 4 mg/kg
Administration: Intraperitoneal injection (i.p.), once every day for 17 d
Result: Inhibited lung metastasis.
Molecular Weight

522.54

Formula

C26H34O11
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1([C@H]([C@H](O)[C@]2([H])[C@]3(C4)C)O)[C@@]([C@H](C5=O)OC(CC(C)C)=O)([H])[C@@]2([C@@](O5)([H])C[C@@]3([H])C(C)=C(O)C4=O)CO1)OC
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 : ≥ 25 mg/mL (47.84 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 1.9137 mL 9.5686 mL 19.1373 mL
5 mM 0.3827 mL 1.9137 mL 3.8275 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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: ≥ 2.08 mg/mL (3.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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mg/kg

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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 +
% 
+
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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: 98.01%

SDS (251 KB)

COA (254 KB) HNMR (315 KB) LCMS (263 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. 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 1.9137 mL 9.5686 mL 19.1373 mL 47.8432 mL
5 mM 0.3827 mL 1.9137 mL 3.8275 mL 9.5686 mL
10 mM 0.1914 mL 0.9569 mL 1.9137 mL 4.7843 mL
15 mM 0.1276 mL 0.6379 mL 1.2758 mL 3.1895 mL
20 mM 0.0957 mL 0.4784 mL 0.9569 mL 2.3922 mL
25 mM 0.0765 mL 0.3827 mL 0.7655 mL 1.9137 mL
30 mM 0.0638 mL 0.3190 mL 0.6379 mL 1.5948 mL
40 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1961 mL
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Bruceine 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:

Bruceine A25514-31-2Dihydrobrusatol NSC310616NSC310616NSC 310616NSC-310616ParasiteNF-κBp38 MAPKPhosphataseApoptosisNuclear factor-κBNuclear factor-kappaBAntitumorAntiparasiticMIA PaCa-2MDA-MB-2314T1BALB/c nude mouse pancreatic cancer model4T1 xenograft tumor model4T1-luc breast cancer lung metastasis modelpancreatic cancerbreast cancerInhibitorinhibitorinhibit

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