SF 1670是一种PTEN抑制剂(IC 50 = 2 μ M)。PTEN(Phosphatase and Tensin Homolog deleted on Chromosome 10)是一种3-磷酸肌醇磷酸酶,可将PI(3 4 5)P3转化为PI(4 5)P2,从而对抗PI 3-K对PKB/Akt的激活。用SF 1670预处理中性粒细胞导致增强的fMLP-1诱导的PI(3 4 5)P3信号传导效应,例如Akt磷酸化、NADPH氧化酶介导的超氧化物形成、细胞极化、趋化性迁移和吞噬作用。SF1670也抑制CD45(IC50 = 200 nM)。Publications Powered by Bioz See more details on Bioz 1)Cojohari O. 等(2016)。“人类巨细胞病毒诱导Akt的非典型激活,以刺激短寿命单核细胞的存活。“J Virol 90(14):6443-6452.2)Yousefi B. 等(2017)。Balaglitazone通过在白血病细胞中以PPAR 3依赖的方式上调PTEN来逆转P-糖蛋白介导的多药耐药。“Tumor Biology 39(10):1010428317716501.3)Alsina-Sanchés E. 等(2018)。“ALK 1(激活素受体样激酶1)缺失通过PI 3 K(磷脂酰肌醇3-激酶)激活导致小鼠和人类血管增生。“动脉血栓形成和血管生物学38(5):1216-1229.4)Mitchell J.等人(2018)。“结肠抑制磷酸酶和张力蛋白同源物增加结肠炎细菌导致结肠炎的发展在Il 10-/-小鼠。炎症性肠病24(8):1718-1732。
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SF1670 is an inhibitor of PTEN (IC50 = 2 μM). PTEN (Phosphatase and Tensin Homolog deleted on Chromosome 10) is a 3’ phosphoinositide phosphatase that converts PI(3 4 5)P3 to PI(4 5)P2 thus opposing PKB/Akt activation by PI 3-K. Pretreatment of neutrophils with SF1670 leads to enhanced fMLP-1 induced PI(3 4 5)P3 signaling effects such as Akt phosphorylation NADPH oxidase-mediated superoxide formation cell polarization chemotactic migration and phagocytosis. SF1670 also inhibits CD45 (IC50 = 200 nM).Publications Powered by Bioz See more details on Bioz1) Cojohari O. et al. (2016). "Human cytomegalovirus induces an atypical activation of Akt to stimulate the survival of short-lived monocytes." J Virol 90(14): 6443-6452.2) Yousefi B. et al. (2017). "Balaglitazone reverses P-glycoprotein-mediated multidrug resistance via upregulation of PTEN in a PPARγ-dependent manner in leukemia cells." Tumor Biology 39(10): 1010428317716501.3) Alsina-SanchÃs E. et al. (2018). "ALK1 (Activin-Receptor Like Kinase 1) Loss Results in Vascular Hyperplasia in Mice and Humans Through PI3K (Phosphatidylinositol 3-Kinase) Activation." Arteriosclerosis thrombosis and vascular biology 38(5): 1216-1229.4) Mitchell J. et al. (2018). "Colonic Inhibition of Phosphatase and Tensin Homolog Increases Colitogenic Bacteria Causing Development of Colitis in Il10-/- Mice." Inflammatory Bowel Diseases 24(8): 1718-1732.