2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. STAT Bcl-2 Family Ser/Thr Kinase Survivin c-Myc Apoptosis Necroptosis CDK
  4. Bruceantinol

Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells.

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

Bruceantinol Chemical Structure

Bruceantinol Chemical Structure

CAS No. : 53729-52-5

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Based on 1 publication(s) in Google Scholar

Bruceantinol Related Antibodies

Top Publications Citing Use of Products

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STAT3 STAT5 STAT6 STAT1

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells[1][2][3].

IC50 & Target

IC50: 2.4 pM (STAT3 DNA-binding ability)[2]
Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.05 μM
Compound: 9e
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]
MCF7 IC50
0.063 μM
Compound: 9e
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]
MDA-MB-231 IC50
0.088 μM
Compound: 9e
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

Bruceantinol (Compound 4) (5-40 μM) shows strong inactivation effect against PepMoV with a minimum inhibitory concentration of 10 μM in C. annuum[1].
Bruceantinol (Compound BOL) (0-100 nM, 24 h) significantly decreases colony formation in a dose-dependent manner across the human CRC cell line panel (HCT116, HCT116 p53-/-, HCA-7, H630 and H630R1)[2].
Bruceantinol (300 nM, 24 h) alters the expression of 25 proteins (p-STAT3, MCL-1, c-Myc, and cleaved caspase-7) in HCT116 cells, in which the STAT3-mediated signal pathway is significantly suppressed[2].
Bruceantinol (30 nM, 0-24 h) inhibits STAT3 phosphorylation in HCT116 cells[2].
Bruceantinol (10-300 nM, 24 h) potently suppresses IL-6-induced activation of STAT3 in CRC cells[2].
Bruceantinol (0-1000 nM, 24 h) significantly decreases expression of MCL-1, c-Myc, and surviving in a dose-dependent manner[2].
Bruceantinol (0-1600 nM, 24-48 h) reduces breast cancer cell (MCF-7 and MDA-MB-231) growth[3].
Bruceantinol (100-400 nM, 24 h) results in a gradual decrease in the number of cells in G0/G1 with a corresponding increase in the cell numbers in S and G2/M in MCF-7 and MDA-MB-231 cells[3].
Bruceantinol (100-400 nM, 10 h) decreases CDK2/4/6 protein levels dependently on the proteasome pathway in MCF-7 and MDA-MB-231 cells[3].

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

Bruceantinol Related Antibodies

Cell Proliferation Assay[2]

Cell Line: HCT116, HCT116 p53-/-, HCA-7, SW480, SW48, SW48G12D, RKO, H630 and H630R1
Concentration: 0, 10, 30, 100 nM
Incubation Time: 24 h
Result: Suppressed cell growth to the greatest extent across the human CRC cell line panel.
In Vivo

Bruceantinol (Compound BOL) (2-4 mg/kg, i.p., thrice per week) inhibits p-STAT3 expression in mice bearing HCT 116 xenografts[2].

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

Animal Model: Athymic nude female mice (6-7 w) bearing HCT 116 xenografts[2]
Dosage: 2 and 4 mg/kg
Administration: Intraperitoneal injection (i.p.) thrice a week
Result: Inhibited p-STAT3 expression 32% and 80% with 2 and 4 mg/kg, respectively.
Exhibited potent suppression of the STAT3-associated targets, c-Myc, and surviving.
Resulted in a significant reduction in Ki67 expression and increased TUNEL staining in a dose-dependdent manner.
Molecular Weight

606.61

Formula

C30H38O13
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

COC([C@]12[C@@]3([H])[C@@]4(CO2)[C@@]([C@H]([C@@H]1O)O)([H])[C@@]5([C@@](C(C)=C(C(C5)=O)O)([H])C[C@@]4([H])OC([C@@H]3OC(/C=C(C)/C(C)(C)OC(C)=O)=O)=O)C)=O
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 : 50 mg/mL (82.43 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 1.6485 mL 8.2425 mL 16.4851 mL
5 mM 0.3297 mL 1.6485 mL 3.2970 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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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 (2.06 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 (2.06 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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
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 1.6485 mL 8.2425 mL 16.4851 mL 41.2126 mL
5 mM 0.3297 mL 1.6485 mL 3.2970 mL 8.2425 mL
10 mM 0.1649 mL 0.8243 mL 1.6485 mL 4.1213 mL
15 mM 0.1099 mL 0.5495 mL 1.0990 mL 2.7475 mL
20 mM 0.0824 mL 0.4121 mL 0.8243 mL 2.0606 mL
25 mM 0.0659 mL 0.3297 mL 0.6594 mL 1.6485 mL
30 mM 0.0550 mL 0.2748 mL 0.5495 mL 1.3738 mL
40 mM 0.0412 mL 0.2061 mL 0.4121 mL 1.0303 mL
50 mM 0.0330 mL 0.1649 mL 0.3297 mL 0.8243 mL
60 mM 0.0275 mL 0.1374 mL 0.2748 mL 0.6869 mL
80 mM 0.0206 mL 0.1030 mL 0.2061 mL 0.5152 mL
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Bruceantinol 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:

Bruceantinol53729-52-5STATBcl-2 FamilySer/Thr KinaseSurvivinc-MycApoptosisNecroptosisCDKProtein Serine-Threonine KinaseMycCyclin dependent kinaseInhibitorinhibitorinhibit

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