Berbamine dihydrochloride

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

Product information

CAS Number: 6078-17-7

Molecular Weight: 681.65

Formula: C37H42Cl2N2O6

Chemical Name: (1S, 14R)-20, 21, 25-trimethoxy-15, 30-dimethyl-7, 23-dioxa-15, 30-diazaheptacyclo[22.6.2.2, .1, .1, .0, .0, ]hexatriaconta-3, 5, 8(34), 9, 11, 18(33), 19, 21, 24(32), 25, 27(31), 35-dodecaen-9-ol dihydrochloride

Smiles: Cl.Cl.CN1CCC2=CC(OC)=C3C=C2[C@@H]1CC1C=CC(=CC=1)OC1=CC(C[C@@H]2C4=C(O3)C(OC)=C(C=C4CCN2C)OC)=CC=C1O

InChiKey: USRXDYNDPPUBSG-KKXMJGKMSA-N

InChi: InChI=1S/C37H40N2O6.2ClH/c1-38-14-12-24-19-32(41-3)33-21-27(24)28(38)16-22-6-9-26(10-7-22)44-31-18-23(8-11-30(31)40)17-29-35-25(13-15-39(29)2)20-34(42-4)36(43-5)37(35)45-33;;/h6-11,18-21,28-29,40H,12-17H2,1-5H3;2*1H/t28-,29+;;/m0../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (146.70 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Liang Y, et al. Berbamine, a novel nuclear factor kappaB inhibitor, inhibits growth and induces apoptosis in human myeloma cells. Acta Pharmacol Sin. 2009 Dec;30(12):1659-65.
2. Meng Z, et al. Berbamine inhibits the growth of liver cancer cells and cancer-initiating cells by targeting Ca2+/calmodulin-dependent protein kinase II. Mol Cancer Ther. 2013 Oct;12(10):2067-77.

Products are for research use only. Not for human use.