HIV Protease

Acquired immunodeficiency syndrome is a chronic disease characterized by multiple life-threatening illnesses caused by a retro-virus, human immunodeficiency virus (HIV). A key therapeutic strategy for HIV infection is highly active antiretroviral therapy (HAART), which is a customized combination of anti-retroviral drugs designed to combat the HIV infection. Among various HAART treatment options, small molecule drugs with HIV protease as a drug target have been found to be effective in the treatment of HIV infection/AIDS.

HIV protease, a homodimeric aspartate protease that is critical to the life cycle of the virus, cleaves newly synthesized polyproteins to produce the mature protein components of an infectious HIV virion. Therefore, HIV protease is a key drug target in designing anti-retroviral drugs for the treatment of HIV/AIDS (acquired immunodeficiency syndrome).

CAS No.	Product Name	Inquiry
1356355-11-7	Saquinavir-[d9] A deuterated squinavir. Saquinavir binds to the active site of the viral protease and prevents cleavage of viral polyproteins, preventing maturation of the virus. Saquinavir inhibits both HIV-1 and HIV-2 proteases.
138483-63-3	L-689502 A potent inhibitor of HIV-l protease (IC50= 1 nM)
14110-64-6	Cytochalasin A It is produced by the strain of Helminthosporium dematioideum, Coriolus vernicipes. It has many biological activities, such as inhibiting cytokinesis reversibly, inhibiting megasophil endocytosis and exocytosis. Cytochalasin A is an HIV protease inhibitor.
1416258-16-6	(±)-BI-D Approximately 2.4-2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160-200 nM, in Psip1 and double-KO cells.
150378-17-9	Indinavir Indinavir is a member of the novel hydroxyaminopentane amide class of HIV-1 protease inhibitors. Indinavir is used as an antiviral.
157810-81-6	Indinavir sulfate Indinavir is a protease inhibitor used as a component of highly active antiretroviral therapy to treat HIV infection and AIDS. It inhibits the HIV-1 protease with an IC50 value of 0.41 nM and Ki value of 0.24 nM. However, indinavir demonstrates up to a 50-fold loss in potency against the HIV-1 protease drug-resistant mutations PRL24I, PRI50V, and PRG73S (Kis = 1.4, 27, and 0.55 nM).
159989-64-7	Nelfinavir An HIV-1 protease inhibitor. It inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
161814-49-9	Amprenavir Amprenavir promotes the specific interactions between the nuclear receptor pregnane X receptor (PXR) and the coactivators SRC-1 and PBP.
166335-18-8	PNU-103017 PNU-103017 is an inhibitor of HIV protease.
174484-41-4	Tipranavir Tipranavir, a nonpeptidic HIV protease inhibitor (NPPI), inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-PI-resistant HIV-1 isolates.
185897-02-3	Indinavir-[d6] Indinavir-[d6] is the labelled analogue of Indinavir, which is a member of the novel hydroxyaminopentane amide class of HIV-1 protease inhibitors. It is used as an antiviral.
192725-39-6	Lopinavir Metabolite M-1 Lopinavir Metabolite M-1 is a major metabolite of Lopinavir.
219944-39-5	Isoescin IA Source from the herbs of Aesculus hippocastanum L.
226700-81-8	Fosamprenavir Calcium Salt HIV protease inhibitor; water soluble prodrug of amprenavir.
2563866-80-6	Indinavir-sulfate-ethanolate Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing Apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CLpro inhibito.
26543-89-5	Hinokinin Hinokinin (Compound 1) is a compound isolated from the stems of Hypoestes aristate. Hinokinin exhibits moderate activity of HIV-1 protease enzyme.
2738376-78-6	Amprenavir-d4-1 Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
313682-08-5	Brecanavir Brecanavir is a tyrosyl-based arylsulfonamide, high-affinity, protease inhibitor (PI) for the treatment of human immunodeficiency virus type-1. This compound potently inhibited HIV-1 in cell culture assays with 50% effective concentrations (EC(50)s) of 0.2 to 0.53 nM and was equally active against HIV strains utilizing either the CXCR4 or CCR5 coreceptor, as was found with other PIs. Brecanavir had a <5-fold increase in EC(50)s against 80% of patient isolates tested and had a greater mean in vitro potency than amprenavir, indinavir, lopinavir, atazanavir, tipranavir, and darunavir.
81907-61-1	Ganoderic acid B Ganoderic acid B (GAB) possesses various pharmaceutical effects and has been used as a chemical marker in quality control of G. lucidum and related products
159989-65-8	Nelfinavir Mesylate Nelfinaviris a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor.

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