1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBerbamine dihydrochlorideCat. No.: HY-N0714ACAS No.: 6078-17-7分式: CHClNO分量: 681.65作靶點(diǎn): NF-B; Autophagy作通路: NF-B; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (73.35 mM;

2、 Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以

3、根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.05 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.05 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3

4、.05 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Berbamine dihydrochloride種 NF-B 抑制劑，具有顯 的抗髓瘤療效。IC50 & Target NF-B Autophagy體外研究 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.體內(nèi)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 您邊的抑制劑師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