hiv-1 iiib

HIV-1 inhibitor-6 (3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo-) is a potent HIV-1 pre-mRNA selective splicing inhibitor that blocks HIV replication.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

L 756423 (L756423) is a novel potent and selective and competitive HIV protease inhibitor with a Ki value of 0.049 nM for HIV-1 PR.L 756423 blocks the spread of HIV(IIIb)-infected MT25 lymphocytes at 0.50-0.1 nM and can be used for the study of Acquired Immunodeficiency Syndrome (AIDS).

Denv-in-5 is an effective and selective dengue virus (DENV) inhibitor with EC50 values of 1.47, 9.23, 7.08, 8.91 μM for denV-I-IV and 0.1512 μM for HIV-1IIIB.

HIV-1 inhibitor-54 is a potent inhibitor of WT HIV-1 (strain IIIB) in MT-4 cells, demonstrating anti-HIV activity with an EC50 of 32 nM. [HIV-1 inhibitor-54 can be used to study viral infections.]

Elvitegravir (JTK-303) is a Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor. The mechanism of action of elvitegravir is as an HIV Integrase Inhibitor, and Cytochrome P450 2C9 Inducer.

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC

D77 is anti-HIV-1 inhibitor. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).

HIV-1inhibitor-74 (compound 10c) is a potent inhibitor of HIV-1, displaying an EC50 of 0.0047 µM against HIV-1IIIB. It exhibits cytotoxic properties and effectively inhibits the activity of WTHIV-1RT with an IC50 of 0.134 µM. Additionally, HIV-1inhibitor-74 demonstrates broad-spectrum anti-HIV-1 activity.

IC-1k is an effective inhibitor of HIV-1, exhibiting anti-viral activity with EC50 values of 2.69 nM against HIV-1IIIB and 97.97 nM against HIV-2 ROD. Additionally, IC-1k has been noted to possess cytotoxic properties.

SAMT-247 is an HIV inhibitor that acts by modifying the nucleocapsid NCp7 region of Gag in infected cells and blocking Gag processing and reducing infectivity.

HIV-1 inhibitor-25 (compound R-12a) is a potent inhibitor of HIV-1 reverse transcription (HIV-1 RT) with an IC50 of 0.1061 nM. It exhibits a high antiviral effect against wild-type HIV-1 (EC50: 13.6 nM) and demonstrates low cytotoxicity (to MT). It also inhibits HIV-1 mutants (L100I, K103 N, Y181C, Y188L, E138K, F227L+V106A) with EC50 values ranging from 0.1961 to 5.8136 μM. HIV-1 inhibitor-25 is useful for studying AIDS.

DENV-IN-6 is a potent inhibitor of DENV (I-IV), demonstrating EC50 values of 17.5, 13.20, 6.8, and 11.41 μM for the inhibition of DENV (I-IV) replication, respectively. Additionally, it exhibits anti-HIV-1 IIIB activity, with an EC50 of 0.0181 µM and a CC50 of 64.92 µM [1].

HIV-1 inhibitor-29 is a potent inhibitor of HIV-1 and acts against HIV-1 IIIB (EC50: 2.18 μM). HIV-1 inhibitor-29 shows high resistance to the F227L V106A strain with an EC50 value of 0.974 μM. HIV-1 inhibitor-29 showed low cytotoxicity against MT-4 cells with a CC50 value of 211 μM. HIV-1 inhibitor-29 can be used in AIDS research.

A3N19 is a potent inhibitor of HIV-1 non-nucleoside reverse transcriptase and is able to act on HIV-1 IIIB (EC50: 3.28 nM).

Oxanosine is an analog of guanosine that has been found in S. capreolus and has diverse biological activities, including antibacterial, antiviral, and anticancer properties. It is active against a variety of bacteria, including S. flexneri, P. mirabilis, and E. coli (MICs = 6.25, 12.5, 25 µg ml, respectively, on peptone, but not nutrient, agar). Oxanosine inhibits replication of the HIV-1 strain IIIb in infected CEM and U937, but not H9, cells (EC50s = 7, 27, and >500 µg ml, respectively). It also inhibits the growth of HeLa human cervical cancer cells (IC50 = 32 µg ml) and reduces tumor growth in a murine L1210 lymphocytic leukemia model.

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

Reverse transcriptase-IN-3, a pyrimidine-5-carboxamide derivative, functions as an inhibitor of HIV-1, demonstrating potent activity against both wild-type and mutant strains of HIV-1.

HIV-1 inhibitor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (IC50 = 50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains.

HIV-1 Inhibitor-58 (Compound 10c) is a non-nucleoside reverse transcriptase inhibitor with broad-spectrum antiviral properties, effective against both wild-type strain IIIB and NNRTI-resistant strains like K103N and E138K in MT-4 cells at an EC50 of less than 50 nM. Additionally, it inhibits CYP2C9 and CYP2C19 with IC50 values of 2.06 μM and 1.91 μM, respectively. This compound is utilized in HIV infection research [1].

Zinlirvimab is a humanized IgG1-λ2 monoclonal antibody that neutralizes HIV by targeting the HIV-1 gp120 envelope glycoprotein, specifically the IIIB gp120 V3 loop [1] [2].

F9170, an antiviral peptide derived from the HIV-1 envelope glycoprotein (amino acids 789-803), targets the LLP1 domain in the virus's envelope protein cytoplasmic tail. This interaction inhibits HIV-1 IIIB infection in MT-2 cells, evidenced by an EC50 value of 0.19 µM. Additionally, at a dosage of 3 mg/kg, F9170 significantly lowers plasma viral load in rhesus macaques infected with simian HIV (SHIV).

Cleomiscosins A, B and C exhibit liver-protective properties. Cleomiscosin B shows the potent anti-HIV-1 activity in vitro and also has protective effects on MT4 cells infected by HIV-1(IIIB).