Infection

Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function.

Isodon serra extract (Rabdosia serra extract) is an extract of Isodon serra (Maxim.) Hara, which has antitumor, anti-angiogenic, analgesic, anti-tuberculosis, anti-inflammatory, antibacterial and anti-ischemic activities.

Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi. Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity. Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway.

Acridine-9-carboxaldehyde (Acridine-9-carbaldehyde) is a bioactive compound with potential antibacterial and antitumor activities. Acridine-9-carboxaldehyde is widely used as a building block in compound development to synthesize various bioactive derivatives. Acridine-9-carboxaldehyde exhibits significant cytotoxicity against certain cancer cells, making it an important candidate in cancer inhibition research.

SDH-IN-27 (Compound Q18) is a succinate dehydrogenase inhibitor (SDHI) (IC₅₀: 9.7 mg/L). SDH-IN-27 induces mycelial morphology changes and lipid peroxidation, and exhibits antifungal activity against C. camelliae (EC₅₀: 6.0 mg/L). SDH-IN-27 is an ergosterol biosynthesis inhibitor (EBI) that binds to the active site of CYP51, ultimately leading to cell death of pathogenic fungi.

NNRT-IN-13 is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor that directly inhibiting HIV-1 reverse transcriptase (IC₅₀ = 0.25 μM). NNRT-IN-13 exhibits excellent antiviral activity against wild-type HIV-1 (EC₅₀ = 0.0046 μM) and a broad spectrum of drug-resistant mutants. NNRT-IN-13 exhibits favorable in vivo metabolic and safety profiles. NNRT-IN-13 can be used for human immunodeficiency virus (HIV) research.

Antibacterial agent 78 (compound 30) is an antibacterial agent.

Galbinic acid (α-Acetylsalazinic acid), a lichen acid, shows antibacterial activities against the Gram-positive bacteria B. cereus, B. subtilis, and S. aureus (MICs=62.5, 62.5, 250 μg/ml, respectively). Galbinic acid inhibits the Gram-negative bacterium E. coli (MIC=125 μg/ml).

Dapivirine-d₄ (TMC120-d₄) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.

Epanorin is a secondary metabolite of the Acarospora lichenic species Epanorin can inhibit cancer cells proliferation, ROS production and induce G0/G1 phase arrest. Epanorin shows antibacterial activity. Epanorin can be used for the researches of cancer and infection, such as breast cancer and S. pneumonia infection.

HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC₅₀ value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection.

SARS-CoV-2-IN-108 (Compound 29) is an inhibitor for SARSCoV-2 papain-like protease with an IC₅₀ of 0.14 µM. SARS-CoV-2-IN-108 inhibits the virus replication with an EC₅₀ of 0.21 µM.

ZIKV-IN-5 (compound 5c) is a low-cytotoxicity and acid-stable anti-ZIKV agent (EC₅₀=0.71 μM). ZIKV-IN-5 effectively inhibits the activity of ZIKV NS5 MTase.

SET7-IN-DC21 is a selective, potent SET7 inhibitor (IC₅₀ = 15.93 μM; K_D = 18.00 μM). SET7-IN-DC21 has good selectivity for several other epigenetic targets, such as SUV39H1, G9a, NSD1, DOT1L and MOF. SET7-IN-DC21 can be used for the researches of cancer, infection, inflammation, metabolic and cardiovascular disease, such as breast cancer.

MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC₅₀ value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitory activity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis.

Onc112 acetate is a proline-rich antimicrobial peptide that displays potent activity against Gram-negative bacteria. Onc112 acetate inhibits translation by blocking and destabilizing the initiation complex.

Neuraminidase-IN-5 (Compound 5b) is a potent inhibitor of neuraminidase with an IC₅₀ of 0.02 μM. Neuraminidase (NA) is a promising target for development of anti-influenza agents. Neuraminidase-IN-5 is a dihydrofurocoumarin derivative compound.

N-Acetylnornuciferine is an aporphine alkaloid, whose family members possess potential antibacterial, antiviral, antioxidant, or anticancer activities. N-Acetylnornuciferine can be extracted from the dried roots of Liriodendron tulipifera (American tulip tree, a plant of the Magnoliaceae family) using ethanol.

Caulerpin is an orally active natural product with anti-tumor, anti-viral, anti-oxidant, anti-fungal, anti-bacteria and analgesic activities. Caulerpin acts as an inhibitor of mitochondrial ETC complex I and acetylcholinesterase. Caulerpin blocks hypoxia-induced activation of HIF-1α protein, inhibits VEGF secretion and tumor angiogenesis under hypoxic conditions, reduces the expression of NLRP3 and the production of pro-inflammatory cytokines, and suppresses the load of Mycobacterium tuberculosis. Caulerpin can be used in studies related to breast cancer, prostate cancer, tuberculosis and viral infections.

27-O-Demethylrapamycin, a Rapamycin (HY-10219) derivative, is an antifungal agent. 27-O-Demethylrapamycin inhibits Candida albicans, Saccharomyces cerevisiae, and Fusarium oxysporum.