1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPIK-294Cat. No.: HY-10303CAS No.: 900185-02-6分式: CHNO分量: 489.53作靶點: PI3K作通路: PI3K/Akt/mTOR儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 40 mg/mL (81.71 mM)* means soluble, but saturation

2、unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.0428 mL 10.2139 mL 20.4278 mL5 mM 0.4086 mL 2.0428 mL 4.0856 mL10 mM 0.2043 mL 1.0214 mL 2.0428 mL請根據產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 PIK-294種有效的選擇性 p110 抑制劑，IC50 為 10 nM。IC50 & Target p110 p110 p110 p11010 n

3、M (IC50) 160 nM (IC50) 490 nM (IC50) 10 M (IC50)體外研究Analysis of the specific Class I PI3 Kinase catalytic isoforms p110 (IC50=10 M), p110 (IC50=0.49 M),1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEp110 (IC50=0.01 M) and p110 (IC50=0.16 M) using the inhibitor PIK-294 indicates differential roles

4、inCXCL8-induced neutrophil migration. PIK-294 inhibits both chemokinetic and chemotactic CXCL8-inducedmigration 1. When cells are pre-treated with the PI3K selective inhibitor PIK-294, CXCL8-inducedmigration in the non-gradient and the gradient assay is significantly inhibited. PIK-294 is used at tw

5、oconcentrations 1 M and 10 M. Pre-treatment with 1 M inhibits migration to a greater extent in the non-gradient assay than in the gradient assay. Pre-treatment with 10 M inhibits migration to a significantlygreater extent than the lower dose in both assays. Prior to stimulation with CXCL8, pre-treat

6、ment of the cellswith the PI3K inhibitors, Wortmannin (50 nM), PIK-294 (10 M) and AS-605240 (10 M) for 2 minutes, causea reduction in the phosphorylation of Akt. Pre-treatment of cells prior to stimulation with GM-CSF and theDMSO control with the PI3K inhibitors Wortmannin (50 nM), PIK-294 (10 M) an

7、d AS-605240 (10 M) for 2minutes, reduce the phosphorylation of Akt (p 2.PROTOCOLCell Assay 2 Neutrophils at a concentration of 6106 cells/mL are pre-treated with 1 M and 10 M of the PIK-294 for 30mins prior to the addition of CXCL8 (100 ng/mL) or 0.5 ng/mL GM-CSF. Then a non-gradient or gradient gel

8、assay depending on the type of migration is performed. The gels are then constructed and the migrationstudied 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May19;125(4):733-47.2. Martin KJ, et al. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One. 2015 Feb6;10(2):e0116250.McePdfHeightCaution: Product has not been fully validated for medical ap