E6 Berbamine
E6 Berbamine (Berbamine p-nitrobenzoate) is a potent calmodulin (CaM) antagonist. E6 Berbamine inhibits the activities of calmodulin-dependent myosin light chain kinase (MLCK) and phosphodiesterase (PDE). E6 Berbamine exhibits anti-leukemic activity. E6 Berbamine can be used in research related to cardiovascular abnormalities and chronic myeloid leukemia.
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- CAS. Nr.: 114784-59-7
- Formel: C44H43N3O9
- Molecular Weight:757.83
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
2.13 μM
Compound: 3n
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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
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[PMID: 19285759] |
In Vitro
E6 Berbamine (2 min) acts as a competitive calmodulin (CaM) antagonist, potently inhibiting CaM-activated myosin light chain kinase (MLCK) activity in chicken gastric tissues, with a Ki of 0.95 μM and an IC50 of 8 μM[1].
E6 Berbamine binds directly to dansyl-labeled porcine brain CaM bound to Ca2+, with a Ki of approximately 1 μM[1].
E6 Berbamine inhibits the activity of calmodulin-dependent phosphodiesterase with an IC50 of 0.53 μM[1].
E6 Berbamine (Compound 3n) inhibits the activity of K562 cells with an IC50 value of 2.13 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 114784-59-7
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Molecular Weight 757.83
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Formel C44H43N3O9
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SMILES
COC1=C(OC2=CC3=C(C=C2OC)CCN4C)C5=C(C=C1OC)CCN(C)[C@@]5(CC6=CC=C(C(OC7=CC=C(C=C7)C[C@@]34[H])=C6)OC(C8=CC=C(C=C8)[N+]([O-])=O)=O)[H]
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Synonyms
Berbamine p-nitrobenzoate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (131.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.30 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.30 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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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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.
Reinheit & Dokumentation
Verweise
[1]. Hu ZY, et al. Interaction of berbamine compound E6 and calmodulin-dependent myosin light chain kinase. Biochem Pharmacol. 1992;44(8):1543-1547. [Content Brief]
[2]. Xie J, et al. Berbamine derivatives: a novel class of compounds for anti-leukemia activity. Eur J Med Chem. 2009;44(8):3293-3298. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3196 mL | 6.5978 mL | 13.1956 mL | 32.9889 mL |
| 5 mM | 0.2639 mL | 1.3196 mL | 2.6391 mL | 6.5978 mL | |
| 10 mM | 0.1320 mL | 0.6598 mL | 1.3196 mL | 3.2989 mL | |
| 15 mM | 0.0880 mL | 0.4399 mL | 0.8797 mL | 2.1993 mL | |
| 20 mM | 0.0660 mL | 0.3299 mL | 0.6598 mL | 1.6494 mL | |
| 25 mM | 0.0528 mL | 0.2639 mL | 0.5278 mL | 1.3196 mL | |
| 30 mM | 0.0440 mL | 0.2199 mL | 0.4399 mL | 1.0996 mL | |
| 40 mM | 0.0330 mL | 0.1649 mL | 0.3299 mL | 0.8247 mL | |
| 50 mM | 0.0264 mL | 0.1320 mL | 0.2639 mL | 0.6598 mL | |
| 60 mM | 0.0220 mL | 0.1100 mL | 0.2199 mL | 0.5498 mL | |
| 80 mM | 0.0165 mL | 0.0825 mL | 0.1649 mL | 0.4124 mL | |
| 100 mM | 0.0132 mL | 0.0660 mL | 0.1320 mL | 0.3299 mL |
E6 Berbamine Related Classifications
HY-120997 Related Classifications
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Keywords
- E6 Berbamine
- 114784-59-7
- Berbamine p-nitrobenzoate
- Calmodulin
- Myosin
- Phosphodiesterase (PDE)
- chicken MLCK
- CaM-dependent PDE
- porcine CaM
- cardiovascular abnormalities
- trypsinized MLCK fragments
- chicken gizzards
- imatinib-resistant chronic myelogenous leukemia
- porcine brain CaM
- calmodulin antagonist
- Inhibitor
- inhibitor
- inhibit