NSC727447
Based on 1 Customer Validation
NSC727447 is a vinyl urea-based allosteric inhibitor of HIV reverse transcriptase-associated RNase H with IC50 values of 2.0 μM and 2.5 μM against HIV-1 and HIV-2 RNase H, respectively, and IC50 values of 100 μM and 10.6 μM against Escherichia coli and human RNase H, respectively. NSC727447 exerts allosteric inhibitory effects mainly by interacting with the region adjacent to α-helix I in the thumb subdomain of the p51 subunit of HIV-1 reverse transcriptase. Cys280, Lys281 and the RNase H primer grip region are involved in its action, and it may inhibit the catalytic activity of RNase H by altering the positioning of nucleic acid substrates or the geometry of the RNase H active site. NSC727447 can be used in studies related to HIV infection, the function of HIV reverse transcriptase RNase H, and allosteric inhibition mechanisms.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 95.0%
- No. CAS: 40106-12-5
- Fòrmula: C10H14N2OS
- Peso molecular:210.30
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
HIV-1 RT-associated RNase H 2 μM (IC50) |
HIV-2 RT-associated RNase H 2.5 μM (IC50) |
E. coli RNase H 100 μM (IC50) |
Human RNase H 10.6 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CEM-SS | CC50 |
19.9 μM
Compound: 1
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Cytotoxicity against human CEM-SS cells by XTT assay
Cytotoxicity against human CEM-SS cells by XTT assay
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[PMID: 20547794] |
| CEM-SS | IC50 |
4.3 μM
Compound: 1
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Antiviral activity against HIV-1 isolate RF infected in human CEM-SS cells assessed as inhibition of virus induced cytopathic effect by XTT assay
Antiviral activity against HIV-1 isolate RF infected in human CEM-SS cells assessed as inhibition of virus induced cytopathic effect by XTT assay
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[PMID: 20547794] |
In Vitro
NSC727447 inhibits the RT-associated RNase H activities of HIV-1 and HIV-2 with IC50 values of 2.0 μM and 2.5 μM, respectively, while its IC50 values against E. coli and human RNase H are 100 μM and 10.6 μM, respectively[1].
NSC727447 (50 μM) does not inhibit the RNA-dependent DNA polymerase and pyrophosphorolysis activities of HIV-1 RT, demonstrating preferential inhibitory activity against RNase H function[1].
NSC727447 (0-16 μM) exhibits mutually exclusive inhibition with α-thujaplicinol, an active-site RNase H inhibitor, suggesting that NSC727447 modulates RNase H activity via a mechanism distinct from direct metal chelation[1].
NSC727447 (37 °C; 10 min) inhibits wild-type HIV-1 RT RNase H activity with an IC50 of 1.20 μM, while the p51 thumb C280A mutation reduces its inhibitory sensitivity by approximately 3-fold, supporting the involvement of the p51 thumb in the allosteric action of NSC727447[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 40106-12-5
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Appearance Solid
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Peso molecular 210.30
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Fòrmula C10H14N2OS
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Color Light brown to brown
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SMILES
O=C(C1=C(N)SC2=C1CCCCC2)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (237.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.7551 mL | 23.7756 mL | 47.5511 mL | 118.8778 mL |
| 5 mM | 0.9510 mL | 4.7551 mL | 9.5102 mL | 23.7756 mL | |
| 10 mM | 0.4755 mL | 2.3776 mL | 4.7551 mL | 11.8878 mL | |
| 15 mM | 0.3170 mL | 1.5850 mL | 3.1701 mL | 7.9252 mL | |
| 20 mM | 0.2378 mL | 1.1888 mL | 2.3776 mL | 5.9439 mL | |
| 25 mM | 0.1902 mL | 0.9510 mL | 1.9020 mL | 4.7551 mL | |
| 30 mM | 0.1585 mL | 0.7925 mL | 1.5850 mL | 3.9626 mL | |
| 40 mM | 0.1189 mL | 0.5944 mL | 1.1888 mL | 2.9719 mL | |
| 50 mM | 0.0951 mL | 0.4755 mL | 0.9510 mL | 2.3776 mL | |
| 60 mM | 0.0793 mL | 0.3963 mL | 0.7925 mL | 1.9813 mL | |
| 80 mM | 0.0594 mL | 0.2972 mL | 0.5944 mL | 1.4860 mL | |
| 100 mM | 0.0476 mL | 0.2378 mL | 0.4755 mL | 1.1888 mL |
NSC727447 Related Classifications
HY-W028350 Related Classifications
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Keywords
- NSC727447
- 40106-12-5
- NSC 727447
- NSC-727447
- HIV
- Reverse Transcriptase
- p66 RNase H domain
- HIV-2 reverse transcriptase-associated ribonuclease H
- bacterial RNase H
- HIV-1 RT
- E. coli RNase H
- human RNase H
- HIV-1 reverse transcriptase-associated ribonuclease H
- p51 subunit
- HIV-2 RT
- retroviral RNase H
- Inhibitor
- inhibitor
- inhibit