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RN-18

RN-18是 HIV-1 病毒感染因子的一种拮抗剂。

CAS号

431980-38-0

分子式

C20H16N2O4S

主要靶点

HIV Protease

仅限科研使用

Cat No : CM04608

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Synonyms

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  • CAS No.: 431980-38-0

    RN-18
    CAS#: 431980-38-0

产品信息

RN-18 is an inhibitor of HIV-1 viral infectivity factor (IC50: 6 μM in nonpermissive H9 cells).

CAS号 431980-38-0
分子式 C20H16N2O4S
主要靶点 HIV Protease
主要通路 微生物学|蛋白酶体
分子量 380.42
纯度 99.01%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

nonpermissive H9 cell:6 μM (IC50)

体外活性

RN-18 displays the greater potency (IC50=4.5 μM in CEM cells) and specificity (IC50>100 μM in MT4 cells) among the two compounds. RN-18 and RN-19 show effective 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 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 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. Reverse transcriptase activity in the nonpermissive H9 and CEM cells decreases substantially and in a dose-dependent manner in the presence of the inhibitor RN-18. RN-18 antagonizes the Vif function and inhibits HIV-1 replication only in the presence of A3G [1][2].

溶解度

DMSO:97 mg/mL (254.98mM),Sonification is recommended.

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.

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