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  3. Berbamine dihydrochloride

Berbamine dihydrochloride is an inhibitor of NF-κB activity with remarkable anti-myeloma efficacy.

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

Berbamine dihydrochloride Chemical Structure

Berbamine dihydrochloride Chemical Structure

CAS No. : 6078-17-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Berbamine dihydrochloride:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Berbamine dihydrochloride is an inhibitor of NF-κB activity with remarkable anti-myeloma efficacy.

IC50 & Target[1]

NF-κB

 

Autophagy

 

Cellular Effect
Cell Line Type Value Description References
K562 IC50
11.1 μM
Compound: BBM
Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 35551036]
K562 IC50
17.1 μM
Compound: BBM
Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
[PMID: 35551036]
K562 IC50
8.93 μM
Compound: Berbamine
Cytotoxicity against human imatinib-resistant K562 leukemia cells expressing p210Bcr/Abl and MDR1 at 48 hrs by MTT assay
Cytotoxicity against human imatinib-resistant K562 leukemia cells expressing p210Bcr/Abl and MDR1 at 48 hrs by MTT assay
[PMID: 19285759]
KB ED50
9210 nM
Compound: 23
Cytotoxicity against human KB cells after 72 hrs by SRB assay
Cytotoxicity against human KB cells after 72 hrs by SRB assay
[PMID: 9917283]
U-937 IC50
> 50 μM
Compound: 14, NSC 369310
Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
[PMID: 22766217]
Vero CC50
> 50 μM
Compound: Berbamine
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero IC50
7.87 μM
Compound: Berbamine
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
In Vitro

Berbamine, a novel NF-κB inhibitor, inhibits growth and induces apoptosis in human myeloma cells. Berbamine treatment leads to increased expression of A20, down-regulation of IKKα, p-IκBα, and follows by inhibition of p65 nuclear localization. As a result, NF-κB downstream targets such as cyclin D1, Bcl-xL, Bid and survivin are down-regulated. To determine whether Berbamine has growth inhibitory effect on myeloma cells, KM3 cells are treated with Berbamine at various concentrations for 24, 48, and 72 h, respectively, and then cell viability is assessed by MTT assays. Berbamine inhibits the growth of KM3 cells in a dose- and time-dependent manner, and the IC50 values are 8.17 μg/mL, 5.09 μg/mL, and 3.84 μg/mL for treatment of 24, 48, and 72 h, respectively. In contrast, IC50 value of Berbamine for normal hematopoietic cells is 185.20 μg/mL at 48 h[1].

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

In Vivo

Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbal medicine Berberis amurensis and has been used to treat inflammatory and other diseases.The anti-tumor effects of Berbamine are determined on a xenograft animal model. Two liver cancer cell lines, Huh7 (epithelial) and SK-Hep-1 (mesenchymal-like), are inoculated into NOD/SCID mice by subcutaneous injection. The oral Berbamine treatment greatly suppresses the growth of Huh7 xenografted tumors over the time and leads to a tumor reduction by 70% based on the tumor weight. The growth of SK-Hep-1 cells in NOD/SCID mice is less sensitive to Berbamine than that of Huh7. There is a significant suppression of the growth of the SK-Hep-1 xenograft with more than 50% reduction of the tumor weight[2].

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

Molecular Weight

681.65

Formula

C37H42Cl2N2O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=C(OC2=CC([C@]3([H])CC(C=C4)=CC=C4O5)=C(CCN3C)C=C2OC)C([C@@]6([H])CC7=CC=C(O)C5=C7)=C(CCN6C)C=C1OC.Cl.Cl

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (146.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (36.68 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4670 mL 7.3351 mL 14.6703 mL
5 mM 0.2934 mL 1.4670 mL 2.9341 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 2.08 mg/mL (3.05 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.05 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 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:

Dosage

mg/kg

Animal weight
(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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 96.49%

References
Cell Assay
[1]

The inhibitory effect of Berbamine on growth of KM3 cells is measured by MTT assay. Briefly, KM3 cells (8×103 per well) are incubated with increasing concentrations of Berbamine (1-32 μg/mL) for 24, 48, or 72 h and then pulsed with 20 μL of 5 mg/mL MTT for the last 4 h, 200 μL DMSO is then added to dissolve the formazan crystals. Dye absorbance in viable cells is measured at 570 nm, and then the inhibitory concentration of 50% (IC50) is calculated[1].

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

Animal Administration
[2]

Mice[2]
5×106 Huh7 cells in 50% Matrigel dissolved in PBS are inoculated in a NOD/SCID mice. 5×106 SK-Hep-1 cells are applied for each xenograft without Matrigel. 100 mg/kg of Berbamine is orally treated to mice with a regimen of twice a day for 5 consecutive days after the tumors reach a size of 2 mm in diameter. After 2 days withdraw, the regimen is repeated once[2].

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

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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 1.4670 mL 7.3351 mL 14.6703 mL 36.6757 mL
5 mM 0.2934 mL 1.4670 mL 2.9341 mL 7.3351 mL
10 mM 0.1467 mL 0.7335 mL 1.4670 mL 3.6676 mL
15 mM 0.0978 mL 0.4890 mL 0.9780 mL 2.4450 mL
20 mM 0.0734 mL 0.3668 mL 0.7335 mL 1.8338 mL
25 mM 0.0587 mL 0.2934 mL 0.5868 mL 1.4670 mL
30 mM 0.0489 mL 0.2445 mL 0.4890 mL 1.2225 mL
DMSO 40 mM 0.0367 mL 0.1834 mL 0.3668 mL 0.9169 mL
50 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.7335 mL
60 mM 0.0245 mL 0.1223 mL 0.2445 mL 0.6113 mL
80 mM 0.0183 mL 0.0917 mL 0.1834 mL 0.4584 mL
100 mM 0.0147 mL 0.0734 mL 0.1467 mL 0.3668 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Berbamine dihydrochloride
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