Bavachin-Corylifolin-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBavachinCat. No.: HY-N0233CAS No.: 19879-32-4Synonyms: Corylifolin分式: CHO分量: 324.37作靶點: Estrogen Receptor/ERR作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 150 mg/mL (462.43 mM)

2、* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.0829 mL 15.4145 mL 30.8290 mL5 mM 0.6166 mL 3.0829 mL 6.1658 mL10 mM 0.3083 mL 1.5414 mL 3.0829 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Bavachin從補脂種中分離到的黃酮類物質(zhì)，作為植物雌激素激活雌性激素受體 ER

3、和 ER，EC50 值分別為 320 和 680 nM。IC50 & Target IC50: 320 nM (ER), 680 nM (ER)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Bavachin significantly inhibits melanin synthesis and TYR activity. Bavachin (10 M) inhibits the expressionof TYR and JNK proteins, and the expression of TYR, TRP-1, TRP-2, E

4、RK1, ERK2 and JNK2 mRNA in A375cells. ICI182780 and U0126 cAN significantly reverse the bavachin treatment on the protein expressionlevels and the mRNA expression of TYR, TRP-1, TRP-2, ERK1, ERK2 and JNK2 1. Bavachin accumulateslipid in a dose dependent manner in ORO staining experiments. Bavachin s

5、ignificantly increases the growthof preadipoctye at 10 M compared with the control cells in MTT assay. Bavachin also increases BrdUincorporation into newly synthesized DNA during pre-adipocyte proliferation. BrdU incorporation is enhancedby insulin and further enhanced by co-treatment with insulin a

6、nd bavachin at 2 and 10 M. Bavachinactivates adipogenic factors and increases PPAR transcriptional activity in differentiated adipocytes.Bavachin enhances insulin-stimulated glucose uptake through GLUT4 translocation via Akt and AMPKpathway 2. BVN significantly increases both hMAO-A and hMAO-B activ

7、ities 3. Bavachin shows ER ligandbinding activity in competitive displacement of 3H E2 from recombinant ER. The estrogenic activity ofbavachin is characterized in a transient transfection system using ER or ER and estrogen-responsiveluciferase plasmids in CV-1 cells with an EC50 of 320 nM and 680 nM

8、, respectively. Bavachin increases themRNA levels of estrogen-responsive genes such as pS2 and PR, and decreases the protein level of ER byproteasomal pathway 4.PROTOCOLKinase Assay 3 The chemiluminescent assay is used to confirm PCSEE MAO-A and MAO-B inhibitory effects and to testBNN and BVN hMAO-A

9、 and hMAO-B inhibition using MAO-Glo kit. Each enzymes Arbitrary Light Unit (ALU)is measured in the presence of PCSEE, BNN, BVN, and standard DEP as an MAO-BI positive control.Briefly, hMAO-A and hMAO-B isozymes are diluted to 2 with reaction buffer (pH 7.4) and preincubated with4 PCSEE, BNN, BVN, o

10、r DEP working solutions at RT for 30 min in white opaque 96-well plates. Fordetermining activity inhibition, final 8.5 g/mL concentrations of PCSEE, BNN, BVN, and DEP are used. ForIC50 determination, 8 PCSEE and BNN working solutions are serially diluted using reaction buffers (pH 7.4)to make a 4 co

11、ncentration. Ten points range of PCSEE (1.0 to 250.0 g/mL) and BNN (up to 400 M (135.4g/mL) final concentrations is used. Controls used are with and without ethanol. Ethanol solvent in controlsis kept to a maximum final (volume) of 2%. Each isozyme is substituted with the reaction buffer for theblan

12、k. Based on our preliminary optimizations and Valleys method, the reaction is initiated by adding 4luciferin derivative substrate (LDS) for a final (concentration) of 40 and 4 M for hMAO-A and hMAO-Breactions, respectively. The final volume per well of each reaction is 50 L. The reaction is optimize

13、d for theamount of A and B enzyme used to be incubated for less than 3.5 h at RT. To stop the reaction and producethe luminescence signal RLDR is added to all wells, 50 L to each well, and incubated for a further 30 min.MCE has not independently confirmed the accuracy of these methods. They are for

14、reference only.Cell Assay 1 MTT solution (20 L) is added to each well of the 96-well plates, the cells are cultured for 4 h, the solution isdiscarded, and the purple crystal is dissolved in the wells with 150 L DMSO solution, agitated in a 37Cincubator shaker for 10 min, and the optical density (OD)

15、 is measured at 490 nm by the microplate reader.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. Wang JH, et al. Effects of bavachin and its regulation of melanin synthesis in A375 cells. Biom

16、ed Rep. 2016 Jul;5(1):87-92. Epub 2016May 20.2. Lee H, et al. Bavachin from Psoralea corylifolia Improves Insulin-Dependent Glucose Uptake through Insulin Signaling and AMPKActivation in 3T3-L1 Adipocytes. Int J Mol Sci. 2016 Apr 8;17(4):527.3. Zarmouh NO, et al. Evaluation of the Inhibitory Effects of Bavachinin and Bavachin on Human Monoamine Oxidases A and B. EvidBased Complement Alternat Med. 2015;2015:852194.4. Park J, et al. Activation of Estrogen Receptor by Bavachin from Psoralea cory