Infection

Antileishmanial agent-14 is a sulfuretin analog with potential activity against the parasite Leishmania donovani promastigotes (IC₅₀=4.1 μM). Antileishmanial agent-14 also inhibits infection by L. donovani amastigotes (IC₅₀=11.1 μM).

BING is an antimicrobial peptide that can be isolated from Japanese medaka fish. BING shows a broad-spectrum toxicity against pathogenic bacteria including drug-resistant strains. BING induces a deregulation of periplasmic peptidyl-prolyl isomerases in gram-negative bacteria, and reduces the RNA level of cpxR, which plays a crucial role in the development of antimicrobial resistance.

Artecanin is a SARS-CoV-2 main protease (M^pro) inhibitor with predicted high gastrointestinal absorption and oral bioavailability, and no predicted hepatotoxicity, carcinogenicity, mutagenicity or cytotoxicity. Artecanin interacts with His41 and Cys145, the key amino acid residues in the active site of M^pro, blocks the cleavage and maturation of viral precursor proteins, and forms a stable complex with M^pro. Artecanin blocks the invasion of SARS-CoV-2. Artecanin is applicable to the research of COVID-19.

Maximin 41 is an antimicrobial peptide. Maximin 41 has antibacterial activity against S. aureus (MIC: 75 μg/mL). Maximin 41 has hemolytic activities against human red cells.

Grapefruit Oil Terpeneless is a natural compound extracted from grapefruit, demonstrating profound antimicrobial and antioxidant effects.

KLA peptide acetate is a naturally occurring Antibiotic peptide that is nontoxic outside of cells but is toxic when it enters into the interior of targeted cells. KLA peptide acetate can induce cell Apoptosis by disrupting mitochondrial membranes and activating Caspase. MG1-KLA acetate, formed by the coupling of KLA peptide acetate with MG1, can selectively induce apoptosis in pro-inflammatory microglia. KLA peptide acetate can be used for the research of liver fibrosis. KLA peptide acetate can be used for the research of neonatal hypoxic-ischemic encephalopathy.

Favipiravir-¹³C¹⁵N (T-705-¹³C¹⁵N) is ¹³C and ¹⁵N labeled Favipiravir. Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC₅₀ of 341 nM.

Hydroxyphenyllactic acid-d₃ is the deuterium labeled Hydroxyphenyllactic acid (HY-113219). Hydroxyphenyllactic acid is an antifungal metabolite.

Diacetylsplenopentin (BCH 069) hydrochloride is an antiviral agent, and protects guinea pigs from foot-and-mouth disease (FMD) infection. Berlopentin has immunostimulatory properties.

PLpro-IN-5 (compound 21) is a PLPro protease inhibitor with an IC₅₀ value of 91.14 nM. PLpro-IN-5 shows broad-spectrum antivirus, especially for SARS-CoV, MERS-CoV, SARS-CoV-2.

(5S,8R)-HBV-IN-10 is an enantiomer of compound 6 (WO2021204258A1). Compound 6 is a hepatitis B surface antigen (HBsAg) inhibitor (0.001 μM< EC₅₀ ≤0.05 μM). From patent WO2021204258A1, compound 6.

Mycobactin-IN-2 (compound 49) is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-2 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway.

SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC₅₀: 80 nM). SARS-CoV-2-IN-57 has high affinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively.

SARS-CoV-2-IN-88 (compound 3a) is a potent SARS-CoV-2 inhibitor with inhibitory value of 96.00%.

BVDU 5′-Triphosphate is an antivirus agent with 5′-Triphosphate label, targeting viral DNA polymerase. BVDU 5′-Triphosphate shows excellent selectivity against varicella-zoster virus (VZV) and herpes simplex virus type 1 (HSV-1), due to a specific phosphorylation by the virus-encoded thymidine kinase.

Triclabendazole sulfoxide-¹³C,d₃ is the ¹³C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer.

CM-728 is a oxazepine-naphthoquinone that has cytotoxic and bactericidal effect. CM-728 is a human peroxiredoxin-1 inhibitor. CM-728 is an oxidative stressor that affects mitochondrial function.

CDK9-IN-25 (compound 4a) is an imidazopyrazine CDK9 inhibitor (IC₅₀: 0.24 μM). CDK9-IN-25 has good affinity to the main protease of COVID-19 and has antiviral activity against human coronavirus 229E (IC₅₀: 63.28 μM).

Conofurin-Delta is a potent α7 nAChR inhibitor with an IC₅₀ of 177 nM. Conofurin-Delta also inhibits α9α10 nAChR with an IC₅₀ of 98.1 nM. Conofurin-Delta may be used in SARS-CoV-2 infection research.

SARS-CoV-2-IN-9 is an inhibitor binding to subsites S1 and S2 in SARS-CoV-2 main protease.