RN-18

产品说明书

Print
Chemical Structure| 431980-38-0 同义名 : -
CAS号 : 431980-38-0
货号 : A145644
分子式 : C20H16N2O4S
纯度 : 98%
分子量 : 380.42
MDL号 : MFCD03142961
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(276.01 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 Efficient HIV-1 replication requires the expression of Vif (viral infectivity factor) protein to counter the activity of APOBEC3G (A3G), a DNA-editing cytidine deaminase expressed nonpermissive cells, which catalyzes critical hypermutations in the viral DNA and acts as an innate weapon against retroviruses. In contrast, HIV-1 replication is Vif-independent in host cells that do not express A3G (permissive cells). RN-18 is a small molecule HIV-1 Vif inhibitor with an IC50 of 6 μM in nonpermissive H9 cells. RN-18 also exhibits potent antiviral activity in the nonpermissive CEM cells with IC50 of 4.5 μM but not in permissive MT4 and CEM-SS cells [3]. In 293T cells treated with 50 μM RN-18 for 24 h, Vif protein levels were downregulated, and A3G expression increased, indicating that RN-18 inhibited Vif function and upregulated A3G levels. Similar to A3G, APOBEC3F and APOBEC3C, other members of APOBEC3 family, are also potent inhibitors of HIV-1 replication and is targeted by Vif. The levels of APOBEC3F and APOBEC3C were significantly and quantitatively enhanced in 293T cells treated with 50 μM RN-18 for 24 h [4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL

参考文献

[1]Ali A, Wang J, et al. Synthesis and structure-activity relationship studies of HIV-1 virion infectivity factor (Vif) inhibitors that block viral replication. ChemMedChem. 2012 Jul;7(7):1217-29.

[2]Nathans R, Cao H, et al. Small-molecule inhibition of HIV-1 Vif. Nat Biotechnol. 2008 Oct;26(10):1187-92.

[3]Mohammed I, Parai MK, Jiang X, Sharova N, Singh G, Stevenson M, Rana TM. SAR and Lead Optimization of an HIV-1 Vif-APOBEC3G Axis Inhibitor. ACS Med Chem Lett. 2012 Jun 14;3(6):465-469. doi: 10.1021/ml300037k. PMID: 24533175; PMCID: PMC3922209.

[4]Nathans R, Cao H, Sharova N, Ali A, Sharkey M, Stranska R, Stevenson M, Rana TM. Small-molecule inhibition of HIV-1 Vif. Nat Biotechnol. 2008 Oct;26(10):1187-92. doi: 10.1038/nbt.1496. Epub 2008 Sep 21. PMID: 18806783; PMCID: PMC2693000.