Reverse transcriptase-IN-4
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K. Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
For research use only. We do not sell to patients.
- CAS No.: 3038793-35-7
- Formula: C17H21N5OS
- Molecular Weight:343.45
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
>363.9 μM
Compound: F10
|
Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 36577220] |
In Vitro
Reverse transcriptase-IN-4 (compound F10) (0-10 μM) shows very weak inhibitory effects on all CYP enzymes, and the inhibitory activities of CYP1A2, CYP2D6, CYP3A4T and CYP3A4M exceeds 50 μM. No significant inhibition is observed for CYP2C9 and CYP2C19, with IC50 values of 35.8 μM and 27.1 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 3038793-35-7
-
Molecular Weight 343.45
-
Formula C17H21N5OS
-
SMILES
CC1=CC(C)=CC(C(C2=C(C(NC(SC(C)C)=N2)=O)C)N=[N+]=[N-])=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)