HIV Protease

Doxorubicin hydrochloride is an anthracycline antibiotic with cytotoxic and antitumor activity. It is an effective inhibitor of human DNA topoisomerase I and II, with IC50 values of 0.8 μM and 2.67 μM, respectively. In addition to inhibiting DNA topoisomerases, it can reduce the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase. Doxorubicin hydrochloride also induces apoptosis and autophagy. In animal studies, it is commonly used to induce models of acute renal failure, chronic kidney injury, and heart failure.

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.

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.

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.

Q-VD-OPh is an irreversible caspase inhibitor with an IC50 value of 48 nM against caspase-7 and between 25 and 400 nM against caspase-1, 3, 8, 9, 10, 12. Q-VD-OPh inhibits HIV infection and can cross the blood-brain barrier.

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.

Pepstatin (Pepsin Inhibitor S 735A) is an aspartate protease inhibitor that also inhibits HIV protease activity with specific and oral activity. Pepstatin inhibits autophagy.

Helichrysetin has mild anti-HIV-1 PR activity. Helichrysetin has great potentials for development as an anticancer agent, it has cytotoxic effect on four selected cancer cell lines, A549, MCF-7, Ca Ski, and HT-29.

PDDC inhibitor (Phenyl (R)-(1-(3-(3,4-dimethoxyphenyl)-2,6-dimethylimidazo[1,2-b]pyridazin-8-yl)pyrrolidin-3-yl)carbamate) is a selective and highly potent nSMase2 inhibitor.

3-Deazaadenosine hydrochloride is an inhibitor of S-adenosylhomocysteine hydrolase (Ki: 3.9 µM). It has anti-inflammatory, anti-proliferative, and anti-HIV activity.

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.

Dextran sulfate sodium salt (MW 4500-5500) is a polymer of dehydrated glucose and an inhibitor of complement and coagulation pathways. Dextran sulfate sodium salt (MW 4500-5500) can be used as an anticoagulant, antiviral agent and antilipidemic agent. Dextran sulfate sodium salt (MW 4500-5500) can prevent the HIV-1 virus from adsorbing onto host cells. Dextran sulfate sodium salt (MW 4500-5500) can inhibit NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 4500-5500) can inhibit the immediate blood-mediated inflammatory response (IBMIR).

Baicalin (Baicalein 7-O-β-D-glucuronide) is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.

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]

BRD-6929 is a selective, brain-penetrant HDAC1 and HDAC2 inhibitor (IC50:  1 and 8 nM). BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 (Kis: 0.2 and 1.5 nM) [2]. BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV

Robinetin (3,3',4',5',7-Pentahydroxyflavone) exhibits potent antioxidant and antiradical activities, effectively inhibiting EYPC membrane lipid peroxidation and HbA glycosylation.

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).

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.

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).

Maslinic acid (Crategolic acid) is a DNA polymerase B inhibitor.

(-)-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.

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.

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.

ONX-0914 (PR-957) is a potent and highly specific immunoproteasome inhibitor with minimal cross-reactivity to the constitutive proteasome.