2. NF-κB Apoptosis
  3. RANKL/RANK Apoptosis
  4. Boldine

Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research.

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Boldine Chemical Structure

Boldine Chemical Structure

CAS No. : 476-70-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Boldine:

Boldine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research[1][2][3].

IC50 & Target

OPG/RANKL/RANK[1]
In Vitro

Boldine (10-500 μM, 24 h) inhibits the growth of bladder cancer cells in T24 patients[2].
Boldine (200-500 μM, 24 h) induces cycle arrest and apoptosis of bladder cancer cells in T24 by regulating ERK, AKT and GSK-3β[2].

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

Boldine Related Antibodies

Cell Viability Assay[2]

Cell Line: T24 and RT4
Concentration: 10, 50, 100, 200, 300,400, 500 μM
Incubation Time: 24 h
Result: Inhibited cell growth.

Apoptosis Analysis[2]

Cell Line: T24
Concentration: 200, 400 μM
Incubation Time: 24 h
Result: Caused a G2/M-phase arrest and a marked increase in cell death

Western Blot Analysis[2]

Cell Line: T24
Concentration: 200, 400 μM
Incubation Time: 1,, 3, 24 h
Result: Decreased the level of p-ERK after 24 hours with 200 μM and after 3 and 24 hours with 400 μM.
The anti-p-cdc2 antibody did not demonstrate any difference in the phosphorylation status of cdc2.
Decreased the phosphorylation of GSK-3β after 24 hours at a concentration of 400 μM.
In Vivo

Boldine (50 mg/kg, p.o, for 7 days) attenuates Dextran Sulfate Sodium (DSS) -induced colitis in mice via p65-NF-κB and STAT3 signaling pathways[3].

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

Animal Model: DSS-induced mice model[3]
Dosage: 50 mg/kg
Administration: p.o.
Result: Reduced the expression of CD 68+ and activity of myeloperoxidase (MPO)
Attenuated Pro-Inflammatory Cytokines and the level of malondialdehyde (MDA)
Increased the Activities of Enzymic Antioxidants and Inhibited p65-NF-κB and STAT3 Activity.
Molecular Weight

327.37

Formula

C19H21NO4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=C(OC)C2=C3C(CCN(C)[C@@]3([H])CC4=CC(O)=C(OC)C=C24)=C1
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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (305.46 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 3.0546 mL 15.2732 mL 30.5465 mL
5 mM 0.6109 mL 3.0546 mL 6.1093 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.5 mg/mL (7.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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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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 +
% 
+
%
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0546 mL 15.2732 mL 30.5465 mL 76.3662 mL
5 mM 0.6109 mL 3.0546 mL 6.1093 mL 15.2732 mL
10 mM 0.3055 mL 1.5273 mL 3.0546 mL 7.6366 mL
15 mM 0.2036 mL 1.0182 mL 2.0364 mL 5.0911 mL
20 mM 0.1527 mL 0.7637 mL 1.5273 mL 3.8183 mL
25 mM 0.1222 mL 0.6109 mL 1.2219 mL 3.0546 mL
30 mM 0.1018 mL 0.5091 mL 1.0182 mL 2.5455 mL
40 mM 0.0764 mL 0.3818 mL 0.7637 mL 1.9092 mL
50 mM 0.0611 mL 0.3055 mL 0.6109 mL 1.5273 mL
60 mM 0.0509 mL 0.2546 mL 0.5091 mL 1.2728 mL
80 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9546 mL
100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
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Boldine 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:

Boldine476-70-0RANKL/RANKApoptosisInhibitorBladder cancerDSS-induced mice modelinhibitorinhibit

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