1. Anti-infection Metabolic Enzyme/Protease
  2. HIV Protease HIV
  3. HIV-1 protease-IN-6

HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus.

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HIV-1 protease-IN-6 Chemical Structure

HIV-1 protease-IN-6 Chemical Structure

CAS No. : 2892016-32-7

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Description

HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus[1].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
HEK-293T CC50
> 100 μM
Compound: 17d
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
[PMID: 35483138]
SUP-T1 EC50
0.74 μM
Compound: 17d
Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by
Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by
[PMID: 35483138]
In Vitro

HIV-1 protease-IN-6 (compound 17d) (10 μM; 48 h) exhibits full inhibition against the late stage of HIV-1 replication cycle while the inhibition rate is 2.6% on early stage at the cellular level[1].
HIV-1 protease-IN-6 (10 μM; 24 h) displays antiviral activity against HIV-1NL4-3 with an EC50 value of 0.74 μM, and exhibits anti-DRV-resistant tendency with an EC50 value of 0.61 μM towards DRV-resistant variant[1].

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

Molecular Weight

530.61

Formula

C27H31FN2O6S

CAS No.
SMILES

CC(CN(S(=O)(C1=CC=C(C=C1)F)=O)C[C@H]([C@@H](NC(C2=CC(O)=CC(O)=C2)=O)CC3=CC=CC=C3)O)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
HIV-1 protease-IN-6
Cat. No.:
HY-150549
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