SARS-CoV Inhibitor

Kumatakenin is an orally active apoptosis inducer and autophagy inhibitor, with a K_d value of 2.94 μM for mouse ATG5. Kumatakenin increases the activities of caspase-3, caspase-8 and caspase-9, thereby inducing caspase-dependent apoptosis in ovarian cancer cells. Kumatakenin reduces the expression of chemokines and pro-oncogenic factors in ovarian cancer cells, and inhibits M2 macrophage polarization. Kumatakenin inactivates TRIM65 function, reduces the expression and stability of FASN, and thus inhibits the proliferation, migration, invasion and tumor progression of esophageal cancer cells. Kumatakenin interacts with ATG5 to reduce its protein level, decrease LC3 level, and reduce the number of autophagosomes in the hippocampus. Kumatakenin binds to Eno3 to upregulate its expression, reduce the stability and expression level of IRP1 mRNA, inhibit ferroptosis, alleviate intestinal inflammation, and restore epithelial barrier function. Kumatakenin enhances the efficacy of antibiotics against pathogenic bacteria, inhibits SARS-CoV-2 replication, and reduces cytokine production. Kumatakenin is applicable to research related to ovarian cancer, esophageal cancer, depression and colitis.

Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC₅₀ of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; K_i = 0.04 μM) and SARS-CoV main protease (Mpro).

Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor with blood-brain barrier permeability. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.

Tixagevimab (AZD8895) is a human monoclonal antibody that targets the SARS-CoV-2 receptor binding domain (RBD). It exhibits neutralizing activity against SARS-CoV-2 by binding to the RBD and the S-glycoprotein ectodomain and blocking S-glycoprotein-mediated binding to the receptor.

6-Azuridine (6-Azauridine) is an orally active purine nucleoside analogue. 6-Azuridine activates autophagic flux, induces Apoptosis that depends on AMPK and p53. 6-Azuridine exhibit both antitumor and antiviral activities.

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

2-Thiouridine is an orally active modified nucleobase. 2-Thiouridine stabilizes U:A base pairs and destabilizes U:G wobble base pairs. 2-Thiouridine significantly improves the efficiency and accuracy of nonenzymatic replication of mixed-sequence A/U-containing RNA templates. 2-Thiouridine exhibits antiviral activity against multiple positive-sense single-stranded RNA viruses (DENV2, ZIKV, YFV, JEV, WNV, CHIKV, human coronaviruses ( [HCoV]-229E, HCoV-OC43, SARS-CoV), and MERS-CoV).

Bemnifosbuvir (AT-511) is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₉₀=0.47 μM). Bemnifosbuvir has pangenotypic antiviral activity.

Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a K_i of 14 nM in both enzyme assay and an EC₉₀ of 350 nM in cell-based replicon assay. Boceprevir inhibits SARS-CoV-2 3CL^pro activity.

Bamlanivimab (Anti-Human SARS-CoV-2; LY-CoV555) is an antiviral agent targeting the SARS-CoV-2 spike protein receptor-binding domain (RBD) with a mean K_d of 5.3 nM. Bamlanivimab binds epitopes overlapping the ACE2 binding site on both active and resting RBD conformations, blocks ACE2 attachment, mediates antibody-dependent cell-mediated cytotoxicity, and reduces viral replication and respiratory tract viral load. Bamlanivimab can be used for the research of COVID-19.

Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.09 μM.

Ginkgolic acid C17:1 is a fatty acid synthase (FAS) inhibitor with an IC₅₀ of 10.5 µM. Ginkgolic acid C17:1 shows anti-tumor activity by inhibiting the phosphorylation of STAT3 and inducing apoptosis. Ginkgolic acid C17:1 can block the interaction between S-RBD and ACE2, and has anti-SARS-CoV-2-S pseudovirus activity. Ginkgolic acid C17:1 inhibits the biofilm formation of enterohemorrhagic Escherichia coli and Staphylococcus aureus.

Meplazumab (HcHAb18) is a humanized anti-CD147 IgG1 antibody a K_d of 0.47 nM. Meplazumab shows anti-SARS-CoV-2 and antitumor activity. Meplazumab conjugated with DM1 can form an antibody-conjugated drug ( HcHAb18-DM1), which induces G2/M phase cell cycle arrest and exerts antiproliferative activity in cancer cells. Meplazumab can be used for the researches of COVID-19 pneumonia and non-small cell lung cancer.

TriDAP dihydrochloride (L-Ala-γ-D-Glu-meso-diaminopimelic acid dihydrochloride) is a NOD1 agonist with a K_d value of 34.5 μM. TriDAP dihydrochloride enhances the binding of NOD1-RICK, promotes RICK phosphorylation, and activates the NF-κB, TAK1, MEK/ERK, p38 and interferon response pathways. TriDAP dihydrochloride downregulates Runx2 via increasing ubiquitination and reduces trabecular bone parameters. TriDAP dihydrochloride decreases IκBα levels and increases p65 levels. TriDAP dihydrochloride induces the secretion of proinflammatory mediators IL-8 and prostaglandins, triggers tissue inflammation and innate immune activation, and inhibits SARS-CoV-2 replication in lung epithelial cells. TriDAP dihydrochloride increases the RANKL/OPG ratio in mice, reduces bone mass and enhances osteoclast activity, and inhibits new bone formation by decreasing the mineralization deposition rate in mice. TriDAP dihydrochloride can be used in research related to pulpitis, chronic ulcerative colitis, Crohn's disease and SARS-CoV-2 infection.

Monolaurin (1-Monolaurin) is an orally active antibiotic with antiviral and antibacterial properties.

Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC₅₀=190 nM) via inhibition of SARS-COV-2 3CL pro protease.

Casirivimab (REGN10933) is a human monoclonal antibody that targets the SARS-CoV-2 virus, which causes COVID-19. Casirivimab is ineffective against COVID-19 variants. Casirivimab can be used in combination with Imdevimab (HY-P99342), which alters the lung response of K18-hACE2 mice to the SARS-CoV-2 δ variant, effectively reducing viral load and improving symptoms.

Verbenalin is an orally active terpenoid glycoside that can be extracted from the medicinal plant Verbena officinalis. Verbenalin has anti-inflammatory, antiviral, and neuroprotective effects. Verbenalin has a strong binding affinity to the nsp-12 protein of the SARS-CoV-2 virus. Verbenalin can be used in the research of inflammatory and nervous system diseases such as hepatitis and Alzheimer's disease.

Methylprednisolone (Standard) is the analytical standard of Methylprednisolone. This product is intended for research and analytical applications. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.

Acriflavine (Acriflavinium chloride) hydrochloride is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic agent. Acriflavine hydrochloride is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine hydrochloride inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine hydrochloride is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine hydrochloride is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2.