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PI4KIIIbeta-IN-10

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Chemical Structure| 1881233-39-1 同义名 : -
CAS号 : 1881233-39-1
货号 : A899470
分子式 : C22H25N3O5S2
纯度 : 99%+
分子量 : 475.581
MDL号 : MFCD30187514
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(252.32 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Phosphatidylinositol (PI) are phospholipids that mediate signaling cascades in the cell by binding to effector proteins[2]. Phosphoinositides 4-kinases is a key membrane of the phosphoinositide family, which synthesize phosphatiddylinoditol 4-phosphate (PI4P). Humans have two type II PI4Ks (α and β) and two type III enzymes (α and β)[3]. PI4KIIIβ is critical for mediating viral replication of a number of RNA viruses through the generation of PI4P enriched viral replication platforms. These membranous webs enriched in PI4P play essential roles in spatially concentrating viral replication proteins, and are key in intracellular viral replication[4]. PI4KIIIbeta-IN-10 is a potent inhibitor of PI4KIIIβ with very minor off-target inhibitor of PI4KIIIβ related lipid kinases (IC50 of 3.6 nM). The most potent of these molecules (PI4KIIIbeta-IN-10；compound 10) was screened over a panel of nine related lipid kinases and was >200 fold selective for PI4KIIIβ across all enzymes tested. Two of the most potent and selective molecules (compound 9+10) were also the most effective antiviral compounds in a cellular model of Hepatitis C virus replication, with the best balance of antiviral potency and low cellular toxicity. PI4KIIIbeta-IN-10 shows weak inhibition of PI3KC2γ (IC50 ~1 µM), PI3Kα (~10 µM), and PI4KIIIα (~3 µM), and <20% inhibition at concentrations up to 20 µM for PI4K2α, PI4K2β, and PI3Kβ[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.51mL

2.10mL

1.05mL

21.03mL

4.21mL

2.10mL
参考文献

[1]Rutaganira FU, et al. Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ. J Med Chem. 2016 Mar 10;59(5):1830-9.

[2]Delang, L., Paeshuyse, J., & Neyts, J. The role of phosphatidylinositol 4-kinases and phosphatidylinositol 4-phosphate during viral replication. Biochem Pharmacol. 2012. 84(11), 1400-1408.

[3]Boura, E., & Nencka, R. Phosphatidylinositol 4-kinases: Function, Structure, and Inhibition. Exp Cell Res. 2016. 341(1), 110.

[4]Borawski J, et al. Class III Phosphatidylinositol 4-Kinase Alpha and Beta Are Novel Host Factor Regulators of Hepatitis C Virus Replication. J. Virol. 2009. 83, 10058–10074.

[5]Rutaganira FU, et al. Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ. J Med Chem. 2016. 59(5), 1830-9.