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  3. RN-18

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

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RN-18 Chemical Structure

RN-18 Chemical Structure

CAS No. : 431980-38-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 89 In-stock
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10 mM * 1 mL in DMSO USD 89 In-stock
Solid
5 mg USD 81 In-stock
10 mg USD 130 In-stock
25 mg USD 260 In-stock
50 mg USD 390 In-stock
100 mg USD 600 In-stock
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Description

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

IC50 & Target

IC50: 6 μM (nonpermissive H9 cell)[1]

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM IC50
4.5 μM
Compound: 1, RN-18
Inhibition of X4-tropic HIV-1 LAI Vif infected in CEM cells assessed as inhibition of viral replication incubated for 14 to 21 days measured on every other day by reverse transcriptase assay
Inhibition of X4-tropic HIV-1 LAI Vif infected in CEM cells assessed as inhibition of viral replication incubated for 14 to 21 days measured on every other day by reverse transcriptase assay
[PMID: 24533175]
H9 IC50
6 μM
Compound: 1a; RN-18
Antagonist activity against HIV-1 Vif in human H9 cells expressing A3G assessed as inhibition of viral infection measured after 16 hrs by cell-based assay
Antagonist activity against HIV-1 Vif in human H9 cells expressing A3G assessed as inhibition of viral infection measured after 16 hrs by cell-based assay
[PMID: 27509004]
H9 IC50
6 μM
Compound: 1, RN-18
Inhibition of X4 tropic HIV-1 LAI Vif infected in H9 cells assessed as inhibition of viral replication incubated for 10 to 15 days measured on every second day by reverse transcriptase assay
Inhibition of X4 tropic HIV-1 LAI Vif infected in H9 cells assessed as inhibition of viral replication incubated for 10 to 15 days measured on every second day by reverse transcriptase assay
[PMID: 24533175]
HEK293 EC50
5.8 μM
Compound: RN-18
Inhibition of HIV Vif induced human cytidine-deaminase degradation in double transgenic HEK293 cells constitutively expressing enhanced yellow fluorescent protein expressor (EYFP-A3G) fusion and Tet-Off controllable Vif protein after 24 hrs by fluorimetri
Inhibition of HIV Vif induced human cytidine-deaminase degradation in double transgenic HEK293 cells constitutively expressing enhanced yellow fluorescent protein expressor (EYFP-A3G) fusion and Tet-Off controllable Vif protein after 24 hrs by fluorimetri
[PMID: 19841153]
MT4 IC50
> 100 μM
Compound: 1, RN-18
Inhibition of X4-tropic HIV-1 LAI Vif infected in MT4 cells assessed as inhibition of viral replication incubated for 14 to 21 days measured on every other day by reverse transcriptase assay
Inhibition of X4-tropic HIV-1 LAI Vif infected in MT4 cells assessed as inhibition of viral replication incubated for 14 to 21 days measured on every other day by reverse transcriptase assay
[PMID: 24533175]
In Vitro

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[1]. 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[2].

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

Molecular Weight

380.42

Formula

C20H16N2O4S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=CC=C1OC)C2=CC=CC=C2SC3=CC=C([N+]([O-])=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (262.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6287 mL 13.1434 mL 26.2867 mL
5 mM 0.5257 mL 2.6287 mL 5.2573 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
References
Cell Assay
[2]

H9 or MT4 cells are treated overnight with 0, 1, 5, 10, 25 or 50 μM RN-18 (all at 0.1% DMSO) and infected with HIV-1. All cells are maintained in the presence of DMSO or RN-18 for 14 d, and viral replication is monitored every 2 d by measuring reverse transcriptase activity in culture supernatants. The average % relative infectivity at day 7 is determined from 3 separate reverse transcriptase assays. Grafit software is used to fit curves and to determine IC50[2].

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6287 mL 13.1434 mL 26.2867 mL 65.7168 mL
5 mM 0.5257 mL 2.6287 mL 5.2573 mL 13.1434 mL
10 mM 0.2629 mL 1.3143 mL 2.6287 mL 6.5717 mL
15 mM 0.1752 mL 0.8762 mL 1.7524 mL 4.3811 mL
20 mM 0.1314 mL 0.6572 mL 1.3143 mL 3.2858 mL
25 mM 0.1051 mL 0.5257 mL 1.0515 mL 2.6287 mL
30 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1906 mL
40 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6429 mL
50 mM 0.0526 mL 0.2629 mL 0.5257 mL 1.3143 mL
60 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
80 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8215 mL
100 mM 0.0263 mL 0.1314 mL 0.2629 mL 0.6572 mL
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