Arenavirus Inhibitor

Tecovirimat (ST-246) is an orally bioavailable and selective compound against orthopoxviruses including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC₅₀ values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus.

Losmapimod (GSK-AHAB; GW856553X) is an orally active p38α/β MAPK inhibitor, with pK_i values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity.

AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research.

ARN-75039 is an orally active arenavirus inhibitor. ARN-75039 binds to sites on the GP2 subunit of the mammarenavirus glycoprotein complex, stabilizes prefusion conformation, and blocks viral entry and endosomal membrane fusion to inhibit viral replication and spread. ARN-75039 can be used for the research of lassa fever, arenaviral hemorrhagic fever, and lethal Junín virus infection.

Arevirumab (Arevirumab-3) is a pan-lineage neutralizing human monoclonal antibody cocktail (8.9F, 12.1F, 37.D). Arevirumab protects cynomolgus monkeys from severe Lassa fever caused by lineage II and III LASV isolates. Arevirumab is applicable to research related to Lassa fever.

Losmapimod (GSK-AHAB; GW856553X) hydrochloride is an orally active p38α/β MAPK inhibitor, with pK_i values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod hydrochloride reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod hydrochloride reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod hydrochloride blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod hydrochloride overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod hydrochloride inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity.

ZCL278 is a selective Cdc42 inhibitor with K_ds of 6.4 μM in fluorescence titration and 11.4 μM in surface plasmon resonance (SPR) measurement. ZCL278 is able to disrupt the Cdc42-ITSN interaction as well as GTP/GDP binding. ZCL278 has inhibitory effects on various enveloped viruses, but is ineffective against non-enveloped viruses. ZCL278 can be used for the studies of arsenic neurotoxicity and HER2-positive gastric cancer (GC).

LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC₅₀s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively.

ST-193 is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC₅₀ values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.

GP(33-41) TFA, a 9-aa-long peptide, is the optimal sequence of the GP1 epitope of lymphocytic choriomeningitis virus. GP(33-41) TFA can upregulate H-2D^b molecules at the RMA-S (Db Kb) cell surface with a SC₅₀ of 344 nM.

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.

VV261 is an orally active prodrug of 4'-fluorouridine. VV261 inhibits viral RNA-dependent RNA polymerase. VV261 exhibits antiviral activity against CCHFV, SFTSV and LCMV. VV261 can be used in research related to viral infections.

Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC₅₀ of 1.2 ng/mL.

Anti-Mouse PSGL-1/CD162 Antibody (4RA10) is a rat-derived IgG1 κ type antibody inhibitor, targeting to mouse PSGL-1/CD162. Anti-Mouse PSGL-1/CD162 Antibody (4RA10) blocks PSGL signaling and inhibits leukocyte rolling. Anti-Mouse PSGL-1/CD162 Antibody (4RA10) can be used for the researches of inflammation, immunology and infection, such as pneumonia and lymphocytic choriomeningitis virus infection.

Tecovirimat (ST-246) monohydrate is the monohydrate form of Tecovirimat (HY-14805). Tecovirimat monohydrate is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat monohydrate is evaluated against vaccinia, cowpox virus, ectromelia virus with EC₅₀ values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat monohydrate targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat monohydrate exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat monohydrate could be used in the study for orthopoxvirus-induced diseases.

(E)-LHF-535 is the E-isomer of LHF-535. LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC₅₀s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively.

LASV-IN-1 is a Lassa fever virus (LASV) inhibitor. LASV-IN-1 binds with LASV glycoprotein (GP) and promotes virus membrane fusion and infection. LASV-IN-1 can be used for LASV infection research.

ST-193 hydrochloride is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC₅₀ values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.

Tecovirimat-d₄ (ST-246-d₄) is a deuterium-labelled Tecovirimat (HY-14805). Tecovirimat is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC₅₀ values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat could be used in the study for orthopoxvirus-induced diseases.

Anti-LCMV Nucleoprotein Antibody (VL-4) is rat-derived IgG2a κ type antibody inhibitor, targeting to LCMV nucleoprotein. Anti-LCMV Nucleoprotein Antibody (VL-4) reacts with lymphocytic choriomeningitis virus (LCMV) nucleoprotein. Anti-LCMV Nucleoprotein Antibody (VL-4) stain LCMV-infected cell internally with no surface staining. Anti-LCMV Nucleoprotein Antibody (VL-4) can be used for the detections of immunohistochemistry and flow cytometry in LCMV infection.