PF-429242 

PF429242 is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC₅₀ of 175 nM^[1].

10 μM PF-429242 抑制中国仓鼠卵巢细胞中的内源性 SREBP 加工。PF-429242 还下调人胚胎肾 293 细胞中 SRE-荧光素酶报告基因的信号以及培养的 HepG2 细胞中内源性 SREBP 靶基因的表达。在 HepG2 细胞中，PF-429242 抑制胆固醇合成，IC₅₀ 为 0.5 μM^[1]。
添加 PF-429242 (30 μM) 可显著抑制细胞培养液中的感染性病毒滴度和病毒 RNA 拷贝。PF-429242 处理还显示出对人源 HEK-293、Hep G2 和非人灵长类动物源 LLC-MK2 细胞培养液中 DENV2 产量的抑制作用^[2]。
PF-429242 有效阻止原型沙粒病毒淋巴细胞性脉络丛脑膜炎病毒 (LCMV) 和 LASV 对 GPC 的加工，这与该化合物在培养细胞中对 LCMV 和 LASV 的强效抗病毒活性相关^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

在用 PF-429242 处理 24 h 的小鼠中，肝脏 SREBP 靶基因的表达受到抑制，肝脏胆固醇和脂肪酸合成率降低^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

409.56

C₂₅H₃₅N₃O₂

947303-87-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol Exp Ther. 2008 Sep;326(3):801-8.  [Content Brief]

  [2]. Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46.  [Content Brief]

  [3]. Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803.  [Content Brief]