LY 294002是磷脂酰肌醇3-激酶的選擇性細(xì)胞滲透性強(qiáng)效和特異性抑制劑(IC 50 = 1.4 μ M;純化PI 3-激酶)。在50 μ M的濃度下,它不顯著抑制PKC PKA MAP激酶S6激酶EGFrK c-src激酶PI 4-激酶DAG激酶或兔腎ATP酶。誘導(dǎo)細(xì)胞凋亡。在用fMet-Leu-Phe刺激的完整中性粒細(xì)胞中,LY 294002在50 μ M時(shí)完全消除PI 3-激酶活性,而無細(xì)胞毒性。出版物Powered by Bioz See more details on Bioz 1. Coronas-Serna JM Fernánán-Acero T Molina M Cid VJ.人源化酵母為基礎(chǔ)的工具包監(jiān)測磷脂酰肌醇3-激酶活性在單細(xì)胞和群體水平。微生物細(xì)胞2018;5(12):545-54.2。張P步行者M(jìn)C威廉姆斯RS。癲癇發(fā)作誘導(dǎo)的PIP 3水平降低有助于抑制活性,并被丙戊酸挽救。Neurobiol Dis. 2014;62:296-306.3. Ferná necessar-Acero T Rodríguez-Escudero I Vicente F Monteiro MCn Tormo JR Cantizani J et al. A Yeast-Based In Vivo Bioassay to Screen for Class I Phosphatidylinositol 3-Kinase Specific Inhibitors.生物分子篩選雜志。2012;17(8):1018-29.
產(chǎn)品描述
LY294002 is a selective cell permeable potent and specific inhibitor of phosphatidylinositol 3-kinase (IC50 = 1.4 ??M; purified PI 3-kinase). It does not significantly inhibit PKC PKA MAP kinase S6 kinase EGFrK c-src kinase PI 4-kinase DAG kinase or rabbit kidney ATPase at concentrations of 50 ??M. Induces apoptosis. In intact neutrophils stimulated with fMet-Leu-Phe LY294002 completely abolished PI 3-kinase activity at 50 ??M without cell toxicity.Publications Powered by Bioz See more details on Bioz1. Coronas-Serna JM Fern??ndez-Acero T Molina M Cid VJ. A humanized yeast-based toolkit for monitoring phosphatidylinositol 3-kinase activity at both single cell and population levels. Microbial Cell. 2018;5(12):545-54.2. Chang P Walker MC Williams RS. Seizure-induced reduction in PIP3 levels contributes to seizure-activity and is rescued by valproic acid. Neurobiol Dis. 2014;62:296-306.3. Fern??ndez-Acero T Rodr??guez-Escudero I Vicente F Monteiro MCn Tormo JR Cantizani J et al. A Yeast-Based In Vivo Bioassay to Screen for Class I Phosphatidylinositol 3-Kinase Specific Inhibitors. Journal of Biomolecular Screening. 2012;17(8):1018-29.