Bruceine A
Based on 3 publication(s) in Google Scholar
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.
- Purity: 99.89%
- CAS No.: 25514-31-2
- Formula: C26H34O11
- Molecular Weight:522.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Bruceine A
MoreAll Parasite Isoforms
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Biological Activity
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PFKFB4 44 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.082 μM
Compound: 9b
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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
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[PMID: 33289552] |
| HeLa | IC50 |
1.1 μM
Compound: 9b
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Antiproliferative activity against human HeLa cells
Antiproliferative activity against human HeLa cells
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[PMID: 33289552] |
| HL-60 | IC50 |
0.13 μM
Compound: 9b
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Antiproliferative activity against human HL-60 cells
Antiproliferative activity against human HL-60 cells
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[PMID: 33289552] |
| HT-29 | IC50 |
3.1 μM
Compound: 9b
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Antiproliferative activity against human HT-29 cells
Antiproliferative activity against human HT-29 cells
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[PMID: 33289552] |
| LNCaP | ED50 |
96 nM
Compound: 7
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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
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[PMID: 19026551] |
| Lu1 | ED50 |
79 nM
Compound: 7
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Cytotoxicity against human Lu1 cells after 2 days by sulforhodamine B assay
Cytotoxicity against human Lu1 cells after 2 days by sulforhodamine B assay
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[PMID: 19026551] |
| MCF7 | ED50 |
1.5 nM
Compound: 7
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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
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[PMID: 19026551] |
| MCF7 | ED50 |
15 nM
Compound: 7
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Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay
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[PMID: 19026551] |
| MCF7 | IC50 |
0.18 μM
Compound: 9b
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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
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[PMID: 33289552] |
| MDA-MB-231 | IC50 |
0.23 μM
Compound: 9b
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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] |
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.
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Cell Line:MIA PaCa-2 cells; SW1990, PANC-1 and AsPC-1 cells
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Concentration:6.25, 12.5, 25, 50 and 100 nM; 0.08, 0.31, 1.25, 5 and 20 μM
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Incubation Time:24, 48 and 72 h
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Result:Inhibited the growth of adenocarcinoma cell lines MIA PaCa-2, SW1990, PANC-1, and AsPC-1 cells.
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Cell Line:MIA PaCa-2 cells
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Concentration:12.5, 25 and 50 nM
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Incubation Time:24 h
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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.
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Cell Line:MIA PaCa-2 cells
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Concentration:12.5, 25 and 50 nM
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Incubation Time:24 h
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Result:Inhibited the mRNA expression level of PFKFB4 in MIA PaCa-2 cells.
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Cell Line:MDA-MB-231 and 4T1 cells
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Concentration:24 and 48 h
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Incubation Time:24, 48 and 72 h
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Result:Inhibits the proliferation activity of MDA-MB-231 and 4T1 cells.
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Cell Line:MDA-MB-231 and 4T1 cells
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Concentration:30, 60 and 120 nM; 0.3, 0.6 and 1.2 μM
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Incubation Time:24 h
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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.
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.
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Animal Model:BALB/c athymic male nude mice pancreatic cancer model (6 weeks old)[1]
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Dosage:0.02, 0.1, 0.5 mg/kg
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Administration:Intravenous injection (i.v.), once every day for 10 d
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Result:Inhibited tumor growth.
Reduced protein levels of PFKFB4 and GSK3β in tumor tissues.
Reduced PCNA and Ki67 positive cells.
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Animal Model:4T1 xenograft tumor model (female BALB/c mice, 6-8 weeks old, 18-20 g)[2]
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Dosage:2 and 4 mg/kg
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Administration:Intraperitoneal injection (i.p.), once every day for 2 weeks
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Result:Inhibited tumor growth.
Reduced Ki67 proliferation marker staining and p-MEK staining.
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Animal Model:4T1-luc breast cancer lung metastasis model (female BALB/c mice, 6-8 weeks old, 18-20 g)[2]
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Dosage:2 and 4 mg/kg
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Administration:Intraperitoneal injection (i.p.), once every day for 17 d
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Result:Inhibited lung metastasis.
Chemical Information
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CAS No. 25514-31-2
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Appearance Solid
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Molecular Weight 522.54
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Formula C26H34O11
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Color White to off-white
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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
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Synonyms
Dihydrobrusatol; NSC310616
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Microbiol
2023 Jan;8(1):121-134. PMID: 36604514 -
Biochem Pharmacol
Quassinoid analogs exert potent antitumor activity via reversible protein biosynthesis inhibition in human colorectal cancer. [Abstract]2023 Jun:212:115564. PMID: 37116665 -
Chem Biol Drug Des
Bruceine A inhibited breast cancer proliferation and metastasis by inducing autophagy via targeting PI3K-AKT signaling pathway. [Abstract]2024 Jan;103(1):e14398. PMID: 38010171
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhang P, et al. Bruceine A induces cell growth inhibition and apoptosis through PFKFB4/GSK3β signaling in pancreatic cancer. Pharmacol Res. 2021 Jul;169:105658. [Content Brief]
[2]. Li X, et al. Bruceine A: Suppressing metastasis via MEK/ERK pathway and invoking mitochondrial apoptosis in triple-negative breast cancer. Biomed Pharmacother. 2023 Dec;168:115784. [Content Brief]
[3]. Bawm S, et al. In vitro antitrypanosomal activities of quassinoid compounds from the fruits of a medicinal plant, Brucea javanica. Vet Parasitol. 2008 Dec 20;158(4):288-94. [Content Brief]
[4]. Kim JA, et al. NF-kappaB inhibitors from Brucea javanica exhibiting intracellular effects on reactive oxygen species. Anticancer Res. 2010 Sep;30(9):3295-300. [Content Brief]
[5]. Lu C, et al. A novel P38α MAPK activator Bruceine A exhibits potent anti-pancreatic cancer activity. Comput Struct Biotechnol J. 2021 Jun 6;19:3437-3450. [Content Brief]
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 |
- Bruceine A
- 25514-31-2
- Dihydrobrusatol
- NSC310616
- NSC310616
- NSC 310616
- NSC-310616
- Parasite
- NF-κB
- p38 MAPK
- Phosphatase
- Apoptosis
- Antitumor
- Antiparasitic
- MIA PaCa-2
- MDA-MB-231
- 4T1
- BALB/c nude mouse pancreatic cancer model
- 4T1 xenograft tumor model
- 4T1-luc breast cancer lung metastasis model
- pancreatic cancer
- breast cancer
- Inhibitor
- inhibitor
- inhibit