HIV Protease

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.

(S)-(+)-N-3-Benzylnirvanol (ZSN-76403) is a cytochrome P450 CYP2C19 inhibitor with an IC50 value of 0.179 µM that can be used to study HIV infection.

Ancriviroc(CHEMBL336672), an imidoxime with strong antiretroviral activity, is a potent CCR5 inhibitor that can be used to study HIV.

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.

Lenacapavir (GS-6207) is a potent capsid-targeting inhibitor of HIV replication. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

Cepharanthine (NSC-623442), a biscoclaurine alkaloid, suppresses tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and inhibits cytokine production.

Dolutegravir intermediate-1 (1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid) is a new synthetic Dolutegravir intermediate. Dolutegravir is an integrase inhibitor developed for the treatment of human immunodeficiency virus (HIV)-1 infection.

Tenofovir (GS 1278) is an adenine analog REVERSE TRANSC-RIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIVIRAL AGENTS, due to the emergence of ANTIVIRAL DRUG RESISTANCE when it is used alone.

Nandrolone decanoate (19-Nortestosterone decanoate) is the decanoate salt form of nandrolone, an anabolic steroid analog of testosterone with androgenic, anabolic, and erythropoietin stimulating effects. Nandrolone enters the cell and binds to and activates specific nuclear androgen receptors in responsive tissue, including the prostate, seminal vesicles, scrotum, penis, larynx, hair follicles, muscle, and bone.

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.

5-Fluorouracil (5-FU) is a uracil analog, an inhibitor of DNA synthesis. 5-Fluorouracil has antitumor activity and affects pyrimidine synthesis through inhibition of thymidylate synthase. 5-Fluorouracil causes apoptosis and autophagy.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Emtricitabine (FTC) (FTC), a nucleoside reverse transcriptase inhibitor, exhibits inhibition activity against human immunodeficiency virus (HIV) and hepatitis B virus.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

Sennoside A (NSC-112929), a kind of irritant laxative isolated from rhei rhizome, causes purgative actions in the intestine.

Oleanolic Acid (Caryophyllin) is a natural compound with anti-tumor activities, which are widely distributed in plants.

Aloperine exhibits anti-inflammatory, antibacterial, antiviral, and anti-tumor properties.

Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) is a pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults.

Decanedioic acid (Sebacinsaure) is a saturated, straight-chain naturally occurring dicarboxylic acid.

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Dimercaprol (Dicaptol) is an anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisonings.

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.

Cholic acid sodium (SodiumCholate) exhibits a strong spermicidal and antiviral [anti-human immunodeficiency virus (HIV)-1] activity.

Tenofovir alafenamide (GS-7340) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir.

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.

gp120-α4β7 binding inhibitor 11 is an anti-HIV agent. gp120-α4β7 binding inhibitor 11 interferes the binding of HIV associated glycoprotein gp12G with the integrin α4β7 (IC50=1.64nM).

Gamibetal (4-Amino-3-hydroxybutyric Acid) is used as a chiral reagent in the synthesis of antiepileptic and hypotensive drug GABOB and analogues. Also used in the preparation of HIV-1 inhibitors derived from Betulinic Acid (B330250).

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).

HIV-1 Rev (34-50) (HIV-1 rev Protein (34-50)) is a 17 amino acid peptide with anti-HIV-1 activity. HIV-1 Rev (34-50) is derived from the Rev-responsive element-binding domains of Rev in HIV-1.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

(Iso)-Fosdevirine ( (Iso)-GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological disorders such as late-onset epilepsy.

Tat-beclin 1 acetate is a potent inducer of autophagy and interacts with the negative regulator of autophagy, GAPR-1. Tat-beclin 1 acetate decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1).

BMS-488043 is a novel and unique oral small molecule HIV fusion inhibitor that inhibits the attachment of Human Immunodeficiency Virus type 1 (HIV-1) to CD4(+) lymphocytes.BMS-488043 is used for the treatment of immune disorders, infections, and genitourinary disorders, and can be used in the study of HIV infect

Cys-TAT(47-57) acetate is derived from the HIV-1 transactivating protein. Cys-TAT(47-57) acetate is an arginine rich peptide that can penetrate cells.

Apelin-17 (human, bovine) acetate is an endogenous apelin receptor agonist. Potently inhibits forskolin-stimulated cAMP accumulation (pIC50 = 9.94).

Peptide T acetate is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a synthetic octapeptide whose possible mechanism of action is the competitive inhibition of gp120 to the CD4 receptor as well as binding to vasointestinal peptide receptors and inhibiting cytokine action

IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2.

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.

KM-023 is a new second-generation non-nucleoside reverse transcriptase inhibitor for the study of human immunodeficiency virus (HIV) type 1 infection.

HIV-1 Inhibitor 18A (HIV-1 Inhibitor-18A) specifically inhibits the entry of multiple HIV-1 isolates.

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.

I-XW-053 is a capsid targeted HIV-1 replication inhibitor.

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).

P-113 acetate is an antimicrobial peptide (AMP) derived from the human salivary protein histatin 5, shows good safety and efficacy profiles in gingivitis and human immunodeficiency virus (HIV) patients with oral candidiasis.

Talviraline (Bay 10-8979) is an RNA-induced DNA polymerase inhibitor.Talviraline is a potent inhibitor of HIV-1-induced cell killing and HIV-1 replication in a variety of human cell lines, as well as in fresh human peripheral blood lymphocytes and macrophages.

Aplaviroc (AK 602) is a novel and highly potent CCR5 antagonist with antiviral activity that inhibits HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW and can be used in the study of human immunodeficiency virus infection.

Fosdevirine (GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological related disorders such as late-onset epilepsy.

Peldesine (BCX 34) is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase. Peldesine inhibits T-cell proliferation with an IC50 of 800 nM. Peldesine can be used in research on cutaneous T-cell lymphoma, psoriasis and HIV infection.

TAT peptide (YGRKKRRQRRR), originating from the human immunodeficiency virus-1 (HIV-1) transactivator of transcription (TAT), enhances the solubility and production of heterologous proteins[1]. This cell-penetrating peptide demonstrates significant potential in biotechnological applications.