HIV protease-IN-1

HIV protease-IN-1 (compound 1·succinate), a potent non-peptidic inhibitor of HIV protease, is used in AIDS research [1].

HIV-1 protease-IN-1 is a potent inhibitor of HIV-1 protease (IC50: 90 pM). HIV-1 protease-IN-1 has antiviral activity against B-HIV (EC50: 89 nM): HIV-1 protease-IN-1 was able to act on C-HIV strain ZM246 (EC50: 13.59 nM) and C-HIV strain Indie (EC50: 8.23 nM).

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, demonstrating significant antiviral activity against DRV (darunavir) resistant mutants, surpassing its inhibition efficacy against wild-type viruses.

HIV-1 protease-IN-2 is a potent inhibitor of HIV-1 protease (IC50: 2.53 nM) and exhibits antiviral effects against DRV (Darunavir) sensitive and drug-resistant HIV-1 mutants.

HIV-1 protease-IN-5 is an HIV-1 protease inhibitor (IC50: 1.64 nM). HIV-1 protease-IN-5 exhibits significant effects on wild-type and DRV-resistant HIV-1.

HIV-1 protease-IN-4 (Compound II-22), a potent inhibitor of the HIV-1 protease, acts as a prodrug for atazanavir and significantly enhances its bioavailability in rat plasma, achieving a 5-fold increase in the area under the curve (AUC) and a 67-fold increase in concentration at 24 hours (C24) compared to oral administration of atazanavir alone [1].

HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor with an IC50 of 3.52 nM and an EC50 of 37 nM [1].

HIV-1 protease-IN-8 (compound 34b) is a potent inhibitor of the HIV-1 protease enzyme with an IC50 of 0.32 nM. It exhibits IC50 values of 0.29 μM for the wild-type HIV-1 (HIV-1 NL4-3) and 1.90 μM against a drug-resistant variant (HIV-1 MDR), indicating strong antiviral activity against both strains [1].

HIV-1 protease-IN-9 (compound 5b), a potent HIV-1 protease inhibitor, exhibits strong antiviral efficacy with a dissociation constant (K_i) of 0.028 nM and a half-maximal inhibitory concentration (IC_50) of 66.8 nM [1].

HIV-1 protease-IN-10 (Compound 2) exhibits HIV-1 latency reversing activity (IC50: 0.22 μM), selectively binds to the PKCδ C1b domain (IC50: 0.69 μM), and demonstrates stability against esterase-mediated hydrolysis [1].

HIV-1 protease-IN-11 (compound 34a), an HIV-1 protease inhibitor, demonstrates potent inhibition with an IC50 of 0.41 nM and maintains substantial efficacy against a drug-resistant variant [1].

HIV-1 protease-IN-12 (compound 35b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.51 nM, demonstrating efficacy against drug-resistant variants [1].

HIV-1protease-IN-14 (compound 5ae) is an effective inhibitor of HIV-1protease, exhibiting Ki values of 0.28 nM and 56.9 nM against WTHIV-1PR and R41THIV-1PR, respectively. This compound also demonstrates low cytotoxicity.

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.

HIV-1 Nef-IN-1 is an inhibitor of the HIV-1 Nef protein, effectively competing for Nef-SH3Hck interactions (Kd: 6.7 μM).

CDK9-IN-1 is a selective and potent CDK9 inhibitor with antiviral activity used in the study of PRRSV infections.

Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.

ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) (EC50s: 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively). ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels.

PD 099560 is a non-peptide inhibitor of HIV-1 protease, a significant target enzyme in AIDS research.

SM111 inhibits in vitro replication of HIV-1, including strains resistant to reverse transcriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.

Darunavir Ethanolate (UIC 94017) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.

Lopinavir Metabolite M-1, an active metabolite of Lopinavir, effectively inhibits the HIV protease enzyme with a Ki value of 0.7 pM, demonstrating notable antiviral properties in [in vitro] studies.

XM 323 is an inhibitor of clinical isolates of HIV-1 in vitro and represents a novel class of non-peptidyl inhibitors of HIV-1 protease.

ICeD-2, an inducer of cell death, effectively induces the killing of HIV-1 infected cells, a process reliant on HIV-1 protease activity. It significantly inhibits the hydrolysis of Gly-Pro-AMC by dipeptidyl peptidases DPP8 and DPP9, and robustly stabilizes DPP9 in peripheral blood mononuclear cells (PBMCs) [1].