ITI-367
ITI-367 is a HIV-1 inhibitor that targets the nuclear localization signal 1 (NLS-1) of HIV-1 matrix protein and the interaction between HIV-1 pre-integration complex (PIC) and importin-β. ITI-367 inhibits HIV-1 replication at the pre-integration stage, reduces the formation of 2-LTR circles, and sequesters viral DNA in the cytoplasm. ITI-367 can be used for the research of HIV infection.
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- CAS No.: 288246-59-3
- Formule: C16H11F3N2O3
- Masse moléculaire:336.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
ITI-367 (10 μM) specifically inhibits HIV-1 replication in CEM CD4+ T lymphocytes without affecting HTLV-I replication[1].
ITI-367 (0-10 μM) inhibits HIV-1 ADA replication in primary monocyte-derived macrophages in a dose-dependent manner, with an IC50 of 0.05 μM[1].
ITI-367 (0-10 μM) inhibits HIV-1 M1 replication in tonsil-derived primary T lymphocytes in a dose-dependent manner, with an IC50 of 0.7 μM[1].
ITI-367 (0-1 μM; 3 h pre-infection, 12 days post-infection) inhibits the replication of HIV-1 LAI and HIV-1 SF-162 in cultured human tonsillar lymphoid tissues in vitro in a dose-dependent manner without inducing cytotoxicity[1].
ITI-367 (0-10 μM; 8 days post-infection) targets MA NLS-1 to inhibit viral replication in primary monocyte-derived macrophages[1].
ITI-367 (0-10 μM; 2 h) dose-dependently inhibits the binding of HIV-1 PICs to human importin α in cytoplasmic fractions derived from Jurkat cells[1].
ITI-367 (1 μM; 72 h) specifically inhibits HIV-1 nuclear translocation in primary monocyte-derived macrophages[1].
ITI-367 (10 μM; 2 h pre-incubation, 72 h post-infection) inhibits the nuclear translocation of HIV-1 DNA in primary monocyte-derived macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary monocyte-derived macrophages
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Concentration:1 μM
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Incubation Time:72 h post-infection
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Result:Dramatically reduced the amount of 2-LTR circle forms (a marker of nuclear import).
Did not affect the amount of late reverse transcripts (a marker of reverse transcription).
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Cell Line:primary monocyte-derived macrophages
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Concentration:10 μM
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Incubation Time:2 h pre-incubation; 72 h post-infection
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Result:Resulted in substantially less nuclei-localized fluorescent HIV-1 DNA compared to untreated cells, with viral DNA retained in the cytoplasm.
Chemical Information
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CAS No. 288246-59-3
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Masse moléculaire 336.27
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Formule C16H11F3N2O3
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SMILES
O=C1ON=C(N1C2=CC=CC(C(F)(F)F)=C2)C3=C(OC)C=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ITI-367 Related Classifications
HY-182566 Related Classifications
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Keywords
- ITI-367
- 288246-59-3
- ITI367
- ITI 367
- HIV
- importin-β
- CEM CD4+ T lymphocytes
- HTLV-I
- HIV-1 preintegration complex (PIC)
- primary monocyte-derived macrophages
- Jurkat cell-derived cytosolic fractions
- tonsil-derived primary T lymphocytes
- HIV-1 matrix protein (MA)
- nuclear localization signal 1 (NLS-1)
- human tonsil lymphoid tissue
- Inhibitor
- inhibitor
- inhibit