| Bioactivity | PF429242 is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM[1]. |
| Invitro | 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]。 0 --> PF-429242 相关抗体: |
| In Vivo | 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]。 |
| Name | PF-429242 |
| CAS | 947303-87-9 |
| Formula | C25H35N3O2 |
| Molar Mass | 409.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [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. |