Berbamine-dihydrochloride - NF-κB 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBerbamine dihydrochlorideCat. No.: HY-N0714ACAS No.: 6078-17-7分式: CHClNO分量: 681.65作靶点: NF-B; Autophagy作通路: NF-B; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (73.35 mM;

2、 Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.4670 mL 7.3351 mL 14.6703 mL5 mM 0.2934 mL 1.4670 mL 2.9341 mL10 mM 0.1467 mL 0.7335 mL 1.4670 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以

3、根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.05 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.05 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3

4、.05 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Berbamine dihydrochloride种 NF-B 抑制剂，具有显 的抗髓瘤疗效。IC50 & Target NF-B Autophagy体外研究 Berbamine, a novel NF-B inhibitor, inhibits growth and induces apoptosis in human myeloma cells.Berbamine treatment leads to

5、increased expression of A20, down-regulation of IKK, p-IB, and follows byinhibition of p65 nuclear localization. As a result, NF-B downstream targets such as cyclin D1, Bcl-xL, Bidand survivin are down-regulated. To determine whether Berbamine has growth inhibitory effect on myelomacells, KM3 cells

6、are treated with Berbamine at various concentrations for 24, 48, and 72 h, respectively, andthen cell viability is assessed by MTT assays. Berbamine inhibits the growth of KM3 cells in a dose- andtime-dependent manner, and the IC50 values are 8.17 g/mL, 5.09 g/mL, and 3.84 g/mL for treatment of24, 4

7、8, and 72 h, respectively. In contrast, IC50 value of Berbamine for normal hematopoietic cells is 185.20g/mL at 48 h 1.体内研究 Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbalmedicine Berberis amurensis and has been used to treat inflammatory and other

8、 diseases.The anti-tumoreffects 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 subcutaneousinjection. The oral Berbamine treatment greatly suppresses the growth of Huh7 xenog

9、rafted tumors over thetime and leads to a tumor reduction by 70% based on the tumor weight. The growth of SK-Hep-1 cells inNOD/SCID mice is less sensitive to Berbamine than that of Huh7. There is a significant suppression of thegrowth of the SK-Hep-1 xenograft with more than 50% reduction of the tum

10、or weight 2.PROTOCOLCell Assay 1 The inhibitory effect of Berbamine on growth of KM3 cells is measured by MTT assay. Briefly, KM3 cells(8103 per well) are incubated with increasing concentrations of Berbamine (1-32 g/mL) for 24, 48, or 72 hand then pulsed with 20 L of 5 mg/mL MTT for the last 4 h, 2

11、00 L DMSO is then added to dissolve theformazan crystals. Dye absorbance in viable cells is measured at 570 nm, and then the inhibitoryconcentration of 50% (IC50) is calculated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administratio

12、n 2 5106 Huh7 cells in 50% Matrigel dissolved in PBS are inoculated in a NOD/SCID mice. 5106 SK-Hep-1cells are applied for each xenograft without Matrigel. 100 mg/kg of Berbamine is orally treated to mice with aregimen of twice a day for 5 consecutive days after the tumors reach a size of 2 mm in di

13、ameter. After 2 dayswithdraw, the regimen is repeated once 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Liang Y, et al. Berbamine, a novel nuclear factor kappaB inhibitor, inhibits growth and induces apoptosis in human myeloma cells. ActaPharmacol 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-dependentprotein kinase II. Mol Cancer Ther. 2013 Oct;12(10):2