SARS-CoV MPro-IN-1 is a SARS-CoV-2 3CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research[1].
Myrrhone is a terpenoid compound with antiplasmodial effects[1].
2',4'-Dihydroxy-6'-Methoxyacetophenone is a phenolic acetophenone from Artemisia annua. Artemisia annua is an analog of Artemisinin that is effective in the treatment of malaria[1].
Demethoxyencecalin is a chromene isolated from Helianthus annuus, has antifungal activities[1].
CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS[1].
Crexavibart (BMS-986413; C-144-LS) is an IgG1λ2 antibody that targets the SARS-CoV2 spike (S) glycoprotein receptor-binding domain[1].
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.IC50 value: 1.1 μM (for HERG current)Target: PDE3in vitro: HERG current is inhibited by Vesnarinone with an IC50 of 1.1 μM, whereas KvLQT1/minK current is not significantly depressed by Vesnarinone even at 30 μM. The IC50 value for Vesnarinone inhibition of HERG channels is 1 μM. The IC50 for Vesnarinone inhibition of PDE is reported to be 300 μM. [1] Vesnarinone is a novel cytokine inhibitor, for the treatment of lung fibrosis using a murine model of bleomycin (BLM)-induced pulmonary fibrosis. Vesnarinone inhibits BLM-induced pulmonary fibrosis, at least in part, by the inhibition of acute lung injuries in the early phase. [2] Vesnarinone is a new and novel inotropic drug that has unique and complex mechanisms of action. Vesnarinone inhibits phosphodiesterase, thereby leading to increased intracellular calcium, and also affects numerous myocardial ion channels, resulting in the prolongation of the opening time of sodium channels and the decrease in the delayed outward and inward rectifying potassium current. Vesnarinone has also demonstrated significant effects on cytokine production, which may account for some of its observed clinical benefits.[3] Vesnarinone plays an important role in the regulation of cytokines and suggest that the reduction of cytokine release may contribute to the beneficial effects of the drug in the treatment of heart failure. Vesnarinone inhibits the production of TFN-a and IFN-y by LPS stimulated whole blood from patients with heart failure and from healthy volunteers. [4]in vivo: Vesnarinone reduces the circulating levels of TNF-α. Cumulative evidence showed that a variety of cytokine are involved in the pathogenesis of pulmonary fibrosis. [2]
(-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.
Alvircept sudotox is a recombinant CD4 derived from Pneumonas aeruginosa exotoxin A. Alvircept sudotox can be used in the research of HIV infections[1].
Gageotetrin A is an antimicrobial peptide derived from the marine bacterium Bacillus subtilis. Gageotetrin A has antifungal activity, but none toxic to numerous human cancer cells[1].
Benznidazol (Ro 07-1051) is an antiparasitic medication, with an IC50 of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease[1][2].
Febrifugine dihydrochloride is a quinazolinone alkaloid found in the roots and leaves of Dichroa febrifuga, with antimalarial activity[1].
Moxidectin(ProHeart 6; CL301423; Cydectin) is an anthelmintic drug which kills parasitic worms (helminths), and is used for the prevention and control of heartworm and intestinal worms.IC50 value:Target: Anti-parasiticMoxidectin is a semisynthetic derivative of nemadectin, which is produced by fermentation by Streptomyces cyano-griseus. Moxidectin treats and controls some of the most common internal and external parasites by selectively binding to a parasite's glutamate-gated chloride ion channels. These channels are vital to the function of invertebrate nerve and muscle cells; when moxidectin binds to the channels, it disrupts neurotransmission, resulting in paralysis and death of the parasite. Studies of moxidectin show the side effects vary by animal and may be affected by the product’s formulation, application method and dosage.
SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria[1].
Moxifloxacin-d3 is the deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
3α-Akebonoic acid is a α-glucosidase inhibitor with an IC50 value of 0.035 mM. 3α-Akebonoic acid shows antibacterial activity and cytotoxicity[1].
Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h[1].
CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV[1].
Efmarodocokin alfa is a fusion protein of human IL-22 and the IgG4 crystallizable fragment. Efmarodocokin alfa activates IL-22 signaling. Efmarodocokin alfa can be used for the research of severe COVID-19 pneumonia[1].
Lagatide (BN 52080), a heptapeptide, is a short C-terminal analog of sorbin. Lagatide has proabsorptive and antisecretory effect in the different parts of the intestine. Lagatide can be used for the research of chronic diarrhea[1].
Antitubercular agent-19 (Compound 1c) is an antitubercular agent. Antitubercular agent-19 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-19 shows low cytotoxicity and relatively high acute lethal toxicity in BALB/c mice[1].
Albofungin (Antibiotic P-42-1) is isolated from the culture filtrate of Actinomyces tumemacerans strain INMI.P-42. Albofungin shows highly active on a wide variety of gram-positive bacteria and fungi. Albofungin shows cytotoxic to HeLa cell cultures and exhibited antitumor activity on EHRLICH ascites tumor in mice.
Neobritannilactone B, a sesquiterpene, can be isolated from the chloroform fraction of the I. britannica. Neobritannilactone B is cytotoxic. Other extracts of I. britannica are also Dihydrofolate reductase (DHFR) inhibitors, which inhibit Shigella dysenteriae type 1[1][2].
Cbz-Valaciclovir (Benzyloxycarbonyl valacyclovir) can be used to prepare Valaciclovir (HY-17425) and for antiviral research[1].
Cefixime trihydrate (FR-17027 trihydrate) is an antibiotic and a third generation cephalosporin antibiotic, useful for the treatment of a number of bacterial infections[1][2].
RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor. RIPK2-IN-2 can block RIP2-dependent proinflammatory signaling, regulated RIP2 kinase activity in auto inflammatory diseases[1].
LL-25 is a fragment of LL-37 (HY-P1222) but devoid of the immunomodulatory properties of LL-37. LL-25 has antifungal and candidacidal activity[1].
Cefcapene pivoxil hydrochloride hydrate is a prodrug and an orally active 3rd-generation cephalosporin with broad-spectrum of anti-bacterial activity[1]. Cefcapene pivoxil hydrochloride hydrate is used for the study of palmoplantar pustulosis (PPP) and other infectious diseases[2].
SDH-IN-3 is a succinate dehydrogenase (SDH) inhibitor with an IC50 of 7.2 μg/mL. SDH-IN-3 exhibits excellent antifungal activities against Nigrospora oryzae with an EC50 of 1.9 μg/mL. SDH-IN-3 can be used for anti-infection research[1].
Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.