GSK682753A-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK682753ACat. No.: HY-101192CAS No.: 1334294-76-6分式: CHClNO分量: 479.78作靶點(diǎn): EBI2/GPR183作通路: GPCR/G Protein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 : 27 mg/mL (56.28 mM)* means soluble,

2、but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.0843 mL 10.4214 mL 20.8429 mL5 mM 0.4169 mL 2.0843 mL 4.1686 mL10 mM 0.2084 mL 1.0421 mL 2.0843 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 ACTIVITY物活性 GSK682753A是EB病毒誘導(dǎo)受體2 (EBI2) 的反向激動(dòng)劑, IC50值為 53.6 nM。IC50 & T

3、arget IC50: 53.6 nM (EBI2) 1體外研究GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibitionof G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEresponse elem

4、ent-binding protein-based reporter and guanosine5-3-O-(thio)-triphosphate (GTPS) bindingassays, the potency of this compound is 2.6-53.6 nM, and its inhibitory efficacy is 75%. GSK682753A dose-dependently inhibits EBI2 with an IC50of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPSbinding, and

5、 cAMP-response element-binding protein activation with similar potency 1.PROTOCOLCell Assay 1 The effect of GSK682753A on cAMP-induced CREB activation is measured. GSK682753A at varyingconcentrations is added when the transfection is stopped with a DMSO concentration after compoundaddition of 0.1%.

6、The CREB activity is determined 24 h after transfection using the LucLite substrate 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Benned-Jensen T, et al. Ligand modulation of the Epstein-Barr virus-induced seven-transmembrane receptor EBI2: identification of apotent and efficacious inverse agonist. J Biol Chem. 2011 Aug 19;286(33):29292-302.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Te