hiv protease

HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor with an IC50 of 3.52 nM and an EC50 of 37 nM [1].

HIV-1 protease-IN-8 (compound 34b) is a potent inhibitor of the HIV-1 protease enzyme with an IC50 of 0.32 nM. It exhibits IC50 values of 0.29 μM for the wild-type HIV-1 (HIV-1 NL4-3) and 1.90 μM against a drug-resistant variant (HIV-1 MDR), indicating strong antiviral activity against both strains [1].

HIV-1 protease-IN-9 (compound 5b), a potent HIV-1 protease inhibitor, exhibits strong antiviral efficacy with a dissociation constant (K_i) of 0.028 nM and a half-maximal inhibitory concentration (IC_50) of 66.8 nM [1].

HIV-1 protease-IN-11 (compound 34a), an HIV-1 protease inhibitor, demonstrates potent inhibition with an IC50 of 0.41 nM and maintains substantial efficacy against a drug-resistant variant [1].

HIV-1 protease-IN-12 (compound 35b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.51 nM, demonstrating efficacy against drug-resistant variants [1].

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.

(-)-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.

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.

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.

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.

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.

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.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

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).

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.

Ancriviroc (SCH-351125) is an oxime-piperidine compound with strong antiretroviral activity and an orally bioavailable small molecule chemokine receptor CCR5 antagonist (Kd value 9.27nM) that enters HIV-1 through the CCR5 co-receptor and is used to study HIV-1.

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.

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

(2RS)-FPMPA（FPMPA） has antiviral activity with an IC50 value of 1.85 μM measured in human MT12 cells infected with SHIV (DH4R).

HIV-1 inhibitor-54 is a potent inhibitor of WT HIV-1 (strain IIIB) in MT-4 cells, demonstrating anti-HIV activity with an EC50 of 32 nM. [HIV-1 inhibitor-54 can be used to study viral infections.]

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.

INCB-9471 is a CCR5 antagonist with anti-HIV activity and inhibits the interaction between HIV-1 gp120.

Oxindole (Indolin-2-one) is an aromatic heterocyclic building block, and its 2-indolinone derivatives are lead compounds in kinase inhibitor research. The oxindole structure is utilized in receptor tyrosine kinase (RTK) inhibitors, such as SU4984 and intedanib, making the RTK family a significant therapeutic target for anti-cancer drug development.

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).