- 产品描述: RN-18 is a HIV-1 viral infectivity factor (HIV-1 Vif) inhibitor with an IC50 of 6 μM in nonpermissive H9 cells.
- 靶点: IC50: 6 μM (nonpermissive H9 cell);HIVProtease
- 体外研究:
RN-18 and RN-19 exhibits potent antiviral activity in the nonpermissive H9 and CEM cells but not in MT4 or CEM-SS cells, confirming that the antiviral activity was Vif specific. RN-18 shows the greater potency (IC50=4.5 μM in CEM cells) and specificity (IC50>100 μM in MT4 cells) among the two compounds. In the presence of the inhibitor, RN-18, reverse transcriptase activity in the nonpermissive H9 and CEM cells decreases substantially and in a dose-dependent manner. RN-18 also exhibits antiviral activity in CEM-SS modified to stably express A3G but does not exhibit antiviral activity in the parental CEM-SS cell line. RN-18 antagonizes Vif function and inhibits HIV-1 replication only in the presence of A3G. RN-18 increases cellular A3G levels in a Vif-dependent manner and increases A3G incorporation into virions without inhibiting general proteasome-mediated protein degradation. RN-18 enhances Vif degradation only in the presence of A3G, reduces viral infectivity by increasing A3G incorporation into virions and enhances cytidine deamination of the viral genome
- 参考文献:
1. Mohammed I, et al. SAR and Lead Optimization of an HIV-1 Vif-APOBEC3G Axis Inhibitor. ACS Med Chem Lett. 2012 Jun 14;3(6):465-469. 2. Nathans R, et al. Small-molecule inhibition of HIV-1 Vif. Nat Biotechnol. 2008 Oct;26(10):1187-92.
- 溶解性: Soluble in DMSO
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.629 ml 13.143 ml 26.287 ml 5 mM 0.526 ml 2.629 ml 5.257 ml 10 mM 0.263 ml 1.314 ml 2.629 ml 50 mM 0.053 ml 0.263 ml 0.526 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)