Infection

Myristinin B/C is a mixture of Myristinin B and Myristinin C. Myristinin B/C is a flavan compound found in Horsfieldia amygdaline and Myristica cinnamomea. Myristinin B/C can selectively inhibit COX-2 activity with an IC₅₀ of 2.1 μg/mL. Myristinin B/C can reduce the production of prostaglandin E2 (PGE2) and inhibit phospholipase A2 (PLA2), thereby blocking the release of inflammatory mediators. Myristinin B/C can inhibit Candida albicans with an IC₅₀ of 6 μg/mL. Myristinin B/C can be used for the research of inflammation and infection, such as rheumatoid arthritis.

ML267 free base is a blood-brain barrier permeable Antibacterial agent and bacterial phosphopantetheinyl transferase (PPTase) inhibitor, with an IC₅₀ of 0.29 μM against Bacillus subtilis Sfp-PPTase and an IC₅₀ of 8.1 μM against bacterial AcpS-PPTase. ML267 free base attenuates bacterial secondary metabolism, activity, and the production of Sfp-PPTase-dependent metabolites. ML267 free base inhibits the growth of Gram-positive bacteria, including Methicillin (HY-121544)-resistant Staphylococcus aureus. ML267 free base is applicable to research related to bacterial infections, including methicillin-resistant Staphylococcus aureus infections.

Odentegravirum (Odentegravir) is a antiviral agent.

ZIKV-IN-4 (compound 5b) is a low-cytotoxicity and acid-stable anti-ZIKV agent (EC₅₀=3.49 μM). ZIKV-IN-4 effectively inhibits the activity of ZIKV NS5 MTase.

TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity.

Lincomycin-d₃ (U-10149-d₃) is the deuterium labeled Lincomycin. Lincomycin is an orally active lincosamide antibiotic. Lincomycin binds to the ribosomes of Gram-positive bacteria to inhibit protein synthesis. Lincomycin can inhibit chloroplast translation, disrupt chloroplast integrity, and activate chloroplast-to-nucleus retrograde signaling in Arabidopsis thaliana seedlings. Lincomycin induces alterations in lipid profiles and liver injury, disrupts blood glucose and insulin levels, and increases growth rate in mice.

Cys(Npys)-(Arg)9 is a synthetic cationic cell-penetrating peptide with a reversible thiol-reactive nitropyridyl (Npys) group. Cys(Npys)-(Arg)9 efficiently mediates the internalization and delivery of various "cargo" such as proteins and antibodies by forming reversible disulfide bonds with surface-exposed cysteine residues. Cys(Npys)-(Arg)9 endows TALEN proteins with cell-penetrating activity, enabling gene knockout in mammalian cells and protein transduction in wheat microspores. Cys(Npys)-(Arg)9 can be conjugated with antibodies to form cationized IgG for enhancing endosomal escape of oligonucleotides, or form siRNA delivery complexes. When the molar ratio of Cys(Npys)-(Arg)9 to loaded molecules is higher than 1:1, it exerts certain cytotoxic effects on cells. Cys(Npys)-(Arg)9 can be used in studies related to oral squamous cell carcinoma and HIV infection.

SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (K_i=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19.

Enrofloxacin-d₅ (hydriodide) is the deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.

CEF20 is an HLA-A*0201-restricted epitope from cytomegalovirus pp65 (495-503).

HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC₅₀s of 7.3 nM, 9.2 nM and 21.0 nM, respectively.

DNDI-6510 (Compound (S)-x38) is a non-covalent SARS-CoV-2 MPro inhibitor with a IC₅₀ of 0.04 μM. DNDI-6510 has a potent antiviral activity across SARS-CoV-2 and its variants as well as a weak efficacy to SARS-CoV-1. DNDI-6510 significantly improves drug exposure in metabolically humanized mice model (8HUM).

Neuraminidase-IN-3 (compound 23d) is a potent influenza neuraminidase (NA) inhibitor with IC₅₀ values of 0.73, 0.26, and 0.63 nM against H1N1, H5N1, and H5N8 NAs, respectively.

Methyl Clonazepam-d₃ is the deuterium labeled Methylclonazepam (HY-W399186). Methylclonazepam is a benzodiazepine with anxiolytic activity. Methylclonazepam inhibits the absorption of 5-hydroxytryptamine by Schistosoma mansoni. Methylclonazepam derivatives have anti-Schistosoma mansoni activity.

Atanine is an alkaloid with antiparasitic activity. Atanine can be isolated from medicinal plant, Evodia rutaecarpa.

Granaticinic acid is a quinone antibiotic. Granaticinic acid can be found in Streptomyces thermoviolaceus NT1. Granaticinic acid has anti-gram-positive bacterial activity.

S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase ( IC₅₀: 20 nM). The EC₅₀, and CC₅₀ of S 1360 in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants.

Demethoxyviridiol is a mycotoxin originally isolated from N. hinnuleum. Demethoxyviridiol induces lethality in day-old cockerels (LD₅₀=4.2 mg/kg). Demethoxyviridiol is also an inhibitor of phosphatidylinositol 3-kinase (PI3K).

Zedoalactone B is an anti-Babesial agent with an IC₅₀ of 1.6 μg/mL against Babesia gibsoni. Zedoalactone B inhibits NO production with an IC₅₀ of 23.8 μM.

NDM-622 is a Colistin (HY-113678) adjuvant. NDM-622 weakly inhibits IKKβ with an IC₅₀ of 20.40 μM. NDM-622 reduces the minimum inhibitory concentration of colistin against colistin-highly-resistant Acinetobacter baumannii and Klebsiella pneumoniae. NDM-622 decreases bacterial colony-forming units in a mouse peritonitis model infected with colistin-highly-resistant Klebsiella pneumoniae. NDM-622 does not modify bacterial lipid A, induce reactive oxygen species production, or increase bacterial membrane permeability. NDM-622 can be used in the research of extensively drug-resistant Gram-negative bacterial infections, colistin-resistant Acinetobacter baumannii infections, and Klebsiella pneumoniae infections.