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HIV Protease

HIV-1 protease (PR) is a retroviral aspartyl protease (retropepsin), an enzyme involved with peptide bond hydrolysis in retroviruses, that is essential for the life-cycle of HIV, the retrovirus that causes AIDS. HIV protease cleaves newly synthesized polyproteins (namely, Gag and Gag-Pol[3]) at nine cleavage sites to create the mature protein components of an HIV virion, the infectious form of a virus outside of the host cell. Without effective HIV protease, HIV virions remain uninfectious.

  • Doxorubicin hydrochloride
    T102025316-40-9
    Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I II (IC50=0.8 2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.
    • $34
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  • Shikonin
    T1125517-89-5
    Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.
    • $29
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  • Maraviroc
    T6016376348-65-1
    Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.
    • $47
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  • Cosalane
    T23910154212-56-3In house
    Cosalane (NSC 658586) is an HIV replication inhibitor, an inhibitor of chemokine receptor 7 (CCR7) signalling in humans and mice, with antiviral activity that blocks the binding of CCR7 to its natural ligands, CCL19 and CCL21.
    • $462 TargetMol
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  • Chloroquine
    T868954-05-7
    Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.
    • $54
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  • Ro24-7429
    T28578139339-45-0
    Ro24-7429 is an effective and orally active antagonist of HIV-1 transactivator protein Tat and an inhibitor of a runt-related transcription factor 1. Ro24-7429 has anti-HIV, antifibrotic, and anti-inflammatory effects.
    • $84
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  • Scutellarin
    T278927740-01-8
    Scutellarin (Scutellarein-7-glucuronide), an active flavone isolated from Scutellaria baicalensis, can inhibit RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts, and down-regulate the STAT3 Girdin Akt signaling in HCC cells.
    • $45
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  • Pirmitegravir
    T397552245231-10-9In house
    Pirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF p75 binding site. Pirmitegravir inhibits PBMC. Pirmitegravir inhibits PBMC.Pirmitegravir has significant antiviral activity and may be useful in the study of HIV virus infection.
    • $350
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  • Flavopiridol hydrochloride
    T2615131740-09-5
    Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.
    • $44
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  • Q-VD-OPH
    T02821135695-98-5
    Q-VD-OPH (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a pan-caspase inhibitor with potent antiapoptotic properties.
    • $47
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  • Lenacapavir
    T114652189684-44-2
    Lenacapavir (GS-6207) is the first HIV-1 capsid inhibitor approved by the U.S. Food and Drug Administration, the European Medicines Agency, and Health Canada for the treatment of MDR HIV-1 infection.[3]
    • $333
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  • Bis-T-23
    T30479171674-76-3In house
    Bis-T-23 is a promoter of actin-dependent dynamin oligomerization, an HIV-I integrase inhibitor, and a Telstar derivative. Bis-T-23 promotes actin-dependent dynamin oligomerization. Bis-T-23 can be used in studies of HIV and chronic kidney disease (CKD).
    • $350
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  • Kaempferol
    T2177520-18-3
    Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.
    • $46
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  • (S)-(+)-N-3-Benzylnirvanol
    T67926790676-40-3
    (S)-(+)-N-3-Benzylnirvanol is a cytochrome P450 CYP2C19 inhibitor with a ki value of 82.5μM for CYP2C9 and 0.25μM for CYP2C19, which can be used to study HIV infection.
    • $147
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  • Maslinic acid
    T37724373-41-5
    Maslinic acid (Crategolic acid) is a DNA polymerase B inhibitor.
    • $30
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  • 5-Fluorouracil
    T098451-21-8
    5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.
    • $24
    • $30
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  • Azvudine
    T144891011529-10-4
    Azvudine (FNC) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine inhibits NRTI-resistant viral strains. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM).
    • $57
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  • Birinapant
    T60071260251-31-7
    Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.
    • $41
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  • ABBV-744
    T46972138861-99-9In house
    ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.
    • $39
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  • Ingenol mebutate
    TN104775567-37-2
    Ingenol mebutate (Ingenol 3-Angelate) is a potent activator of PKC subtypes including PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM. Ingenol mebutate exhibits antiinflammatory and antitumor activity.
    • $64
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  • Pepstatin
    T369526305-03-3
    Pepstatin (Pepsin Inhibitor S 735A) is an aspartate protease inhibitor that also inhibits HIV protease activity with specific and oral activity. Pepstatin inhibits autophagy.
    • $32
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  • Panobinostat
    T2383404950-80-7
    Panobinostat (NVP-LBH589) is a broad-spectrum HDAC inhibitor (IC50=5 nM) with oral activity and non-selectivity. Panobinostat has antitumor activity and induces apoptosis and autophagy.
    • $32
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  • (-)-Epigallocatechin Gallate
    T2988989-51-5
    (-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.
    • $43
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  • Zingibroside R1
    T496280930-74-1
    Zingibroside R1 (Ginsenoside Z-R1) has anti-HIV-1 activity.
    • $48
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  • Elsulfavirine
    T15210868046-19-9
    Elsulfavirine (VM-1500) is an HIV-1 infection reverse transcriptase inhibitor. It is a new anti-HIV drug.
    • $66
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  • lithospermic acid
    T368328831-65-4
    lithospermic acid is a potent anti-HIV agent and shows anti-gonadotrophic and anti-thyroidal effects.
    • $33
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  • Ebselen
    T082560940-34-3
    Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+ K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.
    • $42
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  • Dextran sulfate sodium salt (MW 4500-5500)
    T136479011-18-1
    Dextran sulfate sodium salt (MW 4500-5500) is an anhydrous glucose polymer with a molecular weight range of 4500-5500. It inhibits human immunodeficiency virus replication by preventing viral adsorption to host cells and is commonly used to model inflammatory bowel disease. The high negative charge from its sulfate groups damages the intestinal mucosal barrier, leading to intestinal barrier dysfunction, macrophage impairment, and bacterial flora disorder.
    • $39
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  • Efavirenz
    T2393154598-52-4
    Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor, acting as a Non-Nucleoside Reverse Transcriptase Inhibitor, Cytochrome P450 3A Inducer, Cytochrome P450 2B6 Inducer, Cytochrome P450 2C9 Inhibitor, Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor, classified as a Non-Nucleoside Analog.
    • $35
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  • AzddMeC
    T2672687190-79-2In house
    AzddMeC (Az-Dcme) is a nucleoside analog with antiviral activity and is an orally active and selective inhibitor of HIV-1 reverse transcriptase and HIV-1 replication.AzddMeC has an EC50 value of 9 nM against HIV-1-infected human PBM cells and 6 nM against HIV-1-infected human macrophages.
    • $71 TargetMol
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  • ST7612AA1
    T706921428535-92-5In house
    ST7612AA1 is a novel potent and oral HDCA inhibitor that acts as an HIV-1 latency reactivator. ST7612AA1 showed significant antitumor activity at low concentrations in vitro and in vivo. ST7612AA1 has potential anticancer activity and can be used to study malaria.
    • $195
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  • Fostemsavir
    T3523864953-29-7
    Fostemsavir (BMS-663068) is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.
    • $61
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  • Cichoric Acid
    TL00066537-80-0
    Cichoric Acid (Dicaffeoyltartaric acid) is a potent inhibitor of human immunodeficiency virus type-1 (HIV-1) integrase and the replication in tissues. It also a class of cannabinomimetics with CB2 receptor-dependent and independent.
    • $35
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  • Andropanolide
    TQ0073869807-57-8
    Andropanolide is a dipterocarbon from Andrographis paniculata with anti-HIV, antimalarial and anticancer activities and inhibits Lipopolysaccharides (LPS)-stimulated overproduction of nitric oxide (NO) in RAW264.7 macrophages.
    • $1,698
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  • 3-Deazaadenosine hydrochloride
    T1011186583-19-9
    3-Deazaadenosine hydrochloride is an inhibitor of S-adenosylhomocysteine hydrolase (Ki: 3.9 µM). It has anti-inflammatory, anti-proliferative, and anti-HIV activity.
    • $128
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  • Nelfinavir Mesylate
    T6001159989-65-8
    Nelfinavir Mesylate (Viracept) is an effective HIV protease inhibitor (Ki: 2 nM).
    • $48
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  • ONX-0914
    T6029960374-59-8
    ONX-0914 (PR-957) is a potent and highly specific immunoproteasome inhibitor with minimal cross-reactivity to the constitutive proteasome.
    • $48
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  • Saquinavir
    T7903127779-20-8
    Saquinavir (Ro 31-8959) is a potent HIV protease inhibitor, is an antiretroviral drug used together with other medications to treat or prevent HIV AIDS.
    • $34
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  • Salaspermic acid
    TN493471247-78-4
    Salaspermic acid, a triterpenoid isolated from the stem bark of Kokoona ochracea, is an inhibitor of HIV reverse transcriptase and HIV replication in H9 lymphocytes, and can be used to study HIV infection.
    • $1,226
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  • Cenicriviroc
    TQ0297497223-25-3
    Cenicriviroc (TAK-652) is an orally active, dual CCR2 CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity.
    • $63
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  • Theaflavin 3,3'-digallate
    T542930462-35-2
    Theaflavin 3,3'-digallate (8-Gingerol) , a major polyphenol found in black tea, is an inducer of oxidative stress which has anti-inflammatory and cancer chemopreventive actions, it reduces tumor angiogenesis by downregulating HIF-1αand VEGF.
    • $84
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  • L 756423
    T24362216863-66-0In house
    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).
    • $390
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  • Cobicistat
    T62461004316-88-4
    Cobicistat (GS-9350) is a carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with which it is used in combination, for the treatment of HIV INFECTIONS.
    • $38
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  • Valproic Acid
    T706499-66-1
    Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.
    • $50
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  • Flavopiridol
    T6837146426-40-6
    Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1 2.
    • $34
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  • Atazanavir sulfate
    T0100229975-97-7
    Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-protease inhibitor used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.
    • $39
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  • Ritonavir
    T1525155213-67-5
    Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.
    • $31
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  • Enfuvirtide acetate
    TP1432914454-00-5
    Enfuvirtide acetate salt is a linear synthetic peptide made of 36 amino acids. It has an acetylated N-terminus and a carboxamide C-terminus.
    • $35
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  • Plerixafor
    T1776110078-46-1
    Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.
    • $42
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  • Baicalin
    T277521967-41-9
    Baicalin (Baicalein 7-O-β-D-glucuronide) is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.
    • $31
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