HIV Inhibitor

Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC₅₀s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.

Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.

Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC₅₀ of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.

Oxindole (Indolin-2-one) is an aromatic heterocyclic building block. 2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.

Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.

Pentosan Polysulfate Sodium is an orally bioavailable, semi-synthetic medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate Sodium also is a potent and selective anti-HIV agent. Pentosan Polysulfate Sodium is used for the treatment of interstitial cystitis.

Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC₅₀s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively. Islatravir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.

Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

Pyrazofurin is an antitumor pyrimidine nucleoside analogue and a orotate-phosphoribosyltransferase inhibitor. Pyrazofurin inhibits cell proliferation and intracellular DNA synthesis by inhibiting uridine 5'-phosphate synthase. Pyrazofurin is also an antibiotic with a broad spectrum of antiviral activity.

DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.

Acetohydroxamic acid is the inhibitor for bacterial and plant urease that can be used for chronic urinary tract infections. Acetohydroxamic acid selectively inhibits arachidonic acid 5-lipoxygenase that is useful in the research of asthma. Acetohydroxamic acid inhibits the formation of advanced glycation end products, and reduces oxidative stress and inflammatory responses. Acetohydroxamic acid exhibits antiviral activity against HIV.

Carrageenan is an antiviral and anticancer agent. Carrageenan inhibits herpes simplex virus (HSV), HIV, and hepatitis A virus (HAV) by directly binding to the viral capsid to block the attachment of viruses such as HPV to HSPG factors on the cell surface. Carrageenan delays and arrests cell cycle progression, exhibits cytotoxicity against HeLa cancer cells, and can be applied to studies related to cervical cancer, genital warts, hepatitis A, and other conditions. Carrageenan also induces acute non-immune inflammation, triggers a three-phase inflammatory response involving the release of multiple proinflammatory mediators, and causes persistent edema, hyperalgesia, and neutrophil recruitment in mice.

Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd, Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.

PYR01 is a non-nucleoside reverse transcriptase inhibitor and a killing activator targeting HIV infected cells. PYR01 has cytokilling and antiviral properties of HIV-1 infection with the IC₅₀ values of 27.5nM and 39.7nM, respectively. PYR01 leads to selective cytotoxicity by promoting HIV-1 Gag-Pol dimerization and HIV-1 protease intracellular activation. PYR01 can be used in the study of HIV.

Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC₅₀s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL^pro activity.

Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

Temsavir (BMS-626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4⁺ T cells.

9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections.

Tenofovir diphosphate disodium is an antiretroviral agent. Tenofovir diphosphate disodium is an inhibitor of HIV reverse transcriptase DNA (K_i = 1.55 μM) and RNA (K_i = 0.022 μM). Tenofovir diphosphate disodium can be used for the research of AIDS.