Virus Protease Inhibitor

Olgotrelvir (STI-1558) sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells.

N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.

Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC₅₀=13 nM).

Aspirin-d₃ is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.

VCH-916 is a thiophene derivative and non-nucleoside inhibitor of HCV NS5B polymerase. VCH-916 binds to Thumb Site II. VCH-916 can be used for the research of hepatitis c virus (hcv) infection.

Tirilazad (U 74006F free base) is a neuroprotective agent. Tirilazad can also bind tightly to the main protease of the COVID-19 virus and exert anti-SARS-CoV-2 activity. Tirilazad scavenges hydroxyl and lipid peroxyl free radicals and maintains the levels of endogenous antioxidants. Tirilazad reduces cerebral infarct volume and improves neurobehavioral scores in animal models of focal ischemia. Tirilazad can be used in research related to ischemic stroke and subarachnoid hemorrhage.

RA-0002034 is a Chikungunya virus (CHIKV) nsP2 protease inhibitor with an IC₅₀ of 58 nM. RA-0002034 covalently modifies the catalytic cysteine in a site-specific manner.

Secutrelvir is an oral SARS-CoV-2 3C-like protease (3CLpro) inhibitor and antiviral agent, with IC₅₀ values of 0.655 nM and 0.697 nM against SARS-CoV-2 3CLpro, respectively. Secutrelvir forms a reversible covalent bond with the catalytic cysteine C145 of SARS-CoV-2 3CLpro, thereby inhibiting viral replication. Secutrelvir exhibits activity against multiple SARS-CoV-2 variants and can be used in research related to coronavirus disease 2019 (COVID-19).

Retro-2 cycl (RN 1-001) is a retrograde transport inhibitor with antiviral activity. Retro-2 cycl (RN 1-001) inhibits JCPyV and HPV16 pseudoviruses, with an IC₅₀ of 54 μM and 160 μM respectively.

JNJ-9676 is an orally active Coronavirus M protein inhibitor and selective Sarbecovirus inhibitor. JNJ-9676 binds to the M protein dimer and forces the protein into an alternative conformational state with a compound-induced binding pocket. JNJ-9676 demonstrates in vitro nanomolar antiviral activity against SARS-CoV-2, SARS-CoV and Sarbecovirus strains from bat and pangolin zoonotic origin.

4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC₅₀ of 13.5 μM.

A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC₅₀ of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.

(-)-Epicatechin gallate (Standard) is the analytical standard of (-)-Epicatechin gallate. This product is intended for research and analytical applications. (-)-Epicatechin gallate (Epicatechin gallate) inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 7.5 μM. (-)-Epicatechin gallate is a GLUT1 and GLUT5 inhibitor. (-)-Epicatechin gallate decreases cell growth of GLUT5-expressing hxt⁰ yeast cells.

Dipotassium glycyrrhizinate (Standard) is the analytical standard of Dipotassium glycyrrhizinate. This product is intended for research and analytical applications. Dipotassium glycyrrhizinate is a HMGB1 inhibitor, inhibits atopic dermatitis-related gene expression with anti-anti-inflammatory activity.

Aloin B (Isobarbaloin) is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC₅₀ of 16.08 μM (hydrolytic activity) and 17.51 μM (deubiquitinase activity). Aloin B is metabolized by rat intestinal flora into aloe-emodin-9-anthrone to exert laxative effects. Aloin B inhibits TPA (HY-18739)-induced ear edema, putrescine elevation, and tumor promotion in mouse skin. Aloin B can be used in research related to anti-inflammation, tumor promotion inhibition, coronavirus disease 2019 (COVID-19) and constipation.

Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies.

AG-7404 is an orally active, irreversible inhibitor of the picornavirus 3C protease. AG-7404 blocks the processing of viral polyproteins, thereby inhibiting viral replication. AG-7404 has synergistic antiviral activity with capsid inhibitors such as V-073 (HY-104074) or BTA798 (HY-106254) and is effective against V-073-resistant variants. AG-7404 is used in the study of enterovirus infections such as poliovirus.

1,8-Dihydroxy-4,5-dinitroanthraquinone (ARDP0006; DHDNE) is a potent inhibitor of serine proteinase NS2B/3, the dengue viral protein. 1,8-Dihydroxy-4,5-dinitroanthraquinone has intermolecular proteinase activity and viral inhibition ability with IC₅₀s of 432 μM and 4.2 μM, respectively. Meanwhile 1,8-Dihydroxy-4,5-dinitroanthraquinone inhibits NS2B/3 cleavage in BHK-21 cells at a dose ranging from 4.2 μM to 432 μM.

Pyridostatin (RR82) trihydrochloride is a G-quadruplex (G4) inducer/stabilizer with a K_d of 490 nM. Pyridostatin trihydrochloride also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC₅₀ of 11.0 μM. Pyridostatin trihydrochloride interacts with G-quadruplex structures, regulates the expression of SRC and SUB1, and induces replication- and transcription-dependent DNA damage, growth arrest, and genomic instability. Pyridostatin trihydrochloride exhibits antiproliferative and antiviral activities. Pyridostatin trihydrochloride can be used in studies related to breast cancer, cervical cancer, and Zika virus infection.

Phenytoin-d₁₀ is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.