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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBaohuoside ICat. No.: HY-N0011CAS No.: 113558-15-9Synonyms: Icariin-II; Icariside-II分式: CHO分量: 514.52作靶點(diǎn): CXCR; Apoptosis作通路: GPCR/G Protein; Immunology/Inflammation; Apoptosis儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6
2、months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 32 mg/mL (62.19 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.9436 mL 9.7178 mL 19.4356 mL5 mM 0.3887 mL 1.9436 mL 3.8871 mL10 mM 0.1944 mL 0.9718 mL 1.9436 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。BIOLOGICAL A
3、CTIVITY物活性 Baohuoside I從朝鮮淫藿中得到的黃酮類化合物,作為 CXCR4 的抑制劑,能夠抑制 CXCR4 的表達(dá),誘導(dǎo)凋亡,具有抗腫瘤活性。IC50 & Target CXCR4 Apoptosis1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Baohuoside I is an inhibitor of CXCR4, and downregulates CXCR4 expression at 12-25 M. Baohuoside I (0-25 M) suppresses NF-B activation i
4、n a dose-dependent manner, suppresses CXCL12 induced the invasionof cervical cancer cells. Baohuoside I also inhibits invasion of breast cancer cells 1. Baohuoside I inhibitsA549 cell viability, with IC50s of 25.1 M at 24 h, 11.5 M and 9.6 M at 48 h and 72 h, respectively.Baohuoside I (25 M) suppres
5、ses the caspase cascade in A549 cells, elevates ROS levels and activatesJNK and p38MAPK signaling cascade 2. Baohuoside I (3.125, 6.25, 12.5, 25.0 and 50.0 g/mL) significantlyand dose-dependently blocks the growth of esophageal squamous cell carcinoma Eca109 cells, with an IC50of 4.8 g/mL at 48 h 3.
6、體內(nèi)研究 Baohuoside I (25 mg/kg) decreases -catenin protein levels, cyclin D1 and survivin expression in nude mice3.PROTOCOLCell Assay 2 The cytotoxicity effect of Baohuoside I on A549 cells is determined by MTT assay. Cells (1104 cells/well)are seeded in a 96-well plate, and treated with Baohuoside I (
7、6.25, 12.5, and 25 M) or 1 mM NAC for 24, 48or 72 h. After MTT containing medium is removed, the crystals that have formed are dissolved by the additionof DMSO to each well. After mixing, the absorbance of the cells is measured at 540 nm by using MultiskanSpectrum Microplate Reader 2.MCE has not ind
8、ependently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Female Balb/c nude mice (4- to 6-weeks-old) are used in the assay. Subconfluent Eca109-Luc cells areharvested and resuspended in PBS to a final density of 2 107 cells/mL. Prior to injection,
9、 cells areresuspended in PBS and analyzed by 0.4% trypan blue exclusion assay (viable cells 90%). Forsubcutaneous injection, 1 107 Eca109-Luc cells in 200 L PBS are injected into the left flank of eachmouse using 27G needles. At 1 week after tumor cell injection, Baohuoside I (25 mg/kg per mouse) is
10、injected intralesionally once a day, whereas the 10 mice intended for vehicle treatment are administered anequal volume of PBS 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kim B, et al. Baohuoside I suppresses invasion of cervical and
11、breast cancer cells through the downregulation of CXCR4 chemokinereceptor expression. Biochemistry. 2014 Dec 9;53(48):7562-9.2. Song J, et al. Reactive oxygen species-mediated mitochondrial pathway is involved in Baohuoside I-induced apoptosis in human non-small cell lung cancer. Chem Biol Interact. 2012 Jul 30;199(1):9-17.3. Wang L, et al. The flavonoid Baohuoside-I inhibits cell growth and downregulates survivin and cyclin D1 expression in esophagealcarcinoma via -catenin-dependent signaling. Oncol Rep. 2011 Nov;26(5):1149-56.McePdfHeightCaution: Prod
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