Infection

Antibacterial agent 107 (compound 14) is a potent antibacterial agent. Antibacterial agent 107 shows potent antibacterial activity against Gram-positive bacteria, with a MIC of 1.56 μg/mL (MRSA). Antibacterial agent 107 exhibits low hemolytic activity, high membrane selectivity, and rapid bactericidal activity. Antibacterial agent 107 shows effective in vivo efficacy in the murine model of bacterial keratitis caused by Staphylococcus aureus ATCC29213.

Succinate dehydrogenase-IN-3 (Ig) is an inhibitor of Succinate dehydrogenase (SDH). Succinate dehydrogenase-IN-3 has antifungal activity.

Anthranilyl-AMSN is a potent PqsA inhibitor, with a K_iapp of 170 nM. Anthranilyl-AMSN decreases HHQ and PQS production. Anthranilyl-AMSN can be used in the research of Pseudomonas aeruginosa infections.

D719 is an HIV-1 integrase inhibitor. D719 binds to the hydrophobic pocket of HIV-1 integrase CCD dimer, disrupts interaction with LEDGF/P75, and prevents integrase nuclear translocation. D719 reduces HIV-1 p24 antigen production in acute infection of human T cells. D719 can be used for the research of HIV infection.

DNA polymerase-IN-4 (Compd 5c), a coumarin derivative, has antiretroviral activity with IC₅₀ value of 134.22 μM.

Sampsone B is a dihydrodibenzodioxinone-type antibacterial agent with a minimum inhibitory concentration (MIC) of ≥128 μg/mL against methicillin-resistant Staphylococcus aureus (MRSA). Sampsone B can be naturally extracted from the aerial parts (stems and leaves) of Hypericum sampsonii.

Jun13698 is a SARS-CoV-2 main protease (M^pro) inhibitor with K_i values of 65.6 nM, 510.0 nM, and 117.5 nM against the wild-type, E166V, and E166A mutants, respectively. Jun13698 forms stable complexes with wild-type and mutant M^pro to mediate enzyme inhibition. Jun13698 exhibits antiviral activity against SARS-CoV-2 variants carrying the E166V/A mutation. Jun13698 is applicable to COVID-19-related research.

CYP51/PD-L1-IN-3 (compound L21) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-3 is a dual inhibitor of CYP51 (IC₅₀: 0.205 μM) and PD-L1 (IC₅₀: 0.039 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-3 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death.

DRGN-1 is an antimicrobial peptide. DRGN-1 exhibits potent antimicrobial and anti-biofilm activities, inhibiting both Gram-negative and Gram-positive bacteria, with an EC₅₀ range of 0.50-4.62 μM. DRGN-1 exerts its antimicrobial effect by disrupting bacterial membrane permeability and slightly depolarizing the membrane potential. DRGN-1 inhibits the formation of biofilms of single bacterial species and mixed species of Pseudomonas aeruginosa and Staphylococcus aureus. DRGN-1 can significantly promote the healing of uninfected and mixed biofilm-infected mouse wounds. DRGN-1 can be used for the study of infections.

Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity.

Sulfameter-d₄ (Sulfametoxydiazine-d₄) is the deuterium labeled Sulfameter (HY-B0213). Sulfameter (Sulfametoxydiazine) is an orally active long-acting sulfonamide antibiotic. Sulfameter is active against both Gram-positive and Gram-negative bacteria. Sulfameter can be used for the research of diseases such as respiratory and urinary tract infections.

4-Piperidinecarboxamide is a mycobacterial aspartyl-tRNA synthetase (AspS) inhibitor. 4-Piperidinecarboxamide is a promising anti-tuberculosis (TB) agent.

Anti-MRSA agent 4 (compound 7a) is a potent and selective growth inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA), with MIC ≤ 0.26 µM. Anti-MRSA agent 4 exhibits no cytotoxic and no hemolytic activity in HEK293 cells.

GSK2236805 is a potent hepatitis C virus inhibitor with pEC₅₀ values of 10.4, 11.1 for HCV genotype 1a (gt1a) and gt1b, respectively.

ANA975, 5-amino-3-β -D-ribofuranosyl-3H-thiazolo[4,5-d]pyrimidin-2-one derivative, is an oral prodrug of the TLR-7 agonist Isatoribine (HY-13655A). ANA975 is converted to Isatoribine via a combined mechanism of hydrolysis by esterases and oxidation by aldehyde oxidase. ANA975 can be used in the research of hepatitis C virus infection.

Antifungal agent 36 is a potent anti-fungal agent. Antifungal agent 36 shows anti-fungal activity for Basidiomycetes.

RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC₅₀ is 54 μM) and VHR (IC₅₀ is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC₅₀s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24[2].

(-)-Maritoclax ((-)-Marinopyrrole A) is an actin-targeting cytotoxic and antibacterial agent. (-)-Maritoclax exhibits cytotoxicity against cancer cells. (-)-Maritoclax can be used in the research of methicillin-resistant Staphylococcus aureus infections and colon cancer.

(S)-BI-1001 (Compound 11) is an active S-enantiomer of BI-1001. (S)-BI-1001 exhibits antiviral potency against HIV-1 integrase with an IC₅₀ of 28 nM, an EC₅₀ of 450 nM and a K_d of 4.7 μM.

Maximin 68 is an antimicrobial peptide. Maximin 68 has antibacterial activity against C. albicans, S. aureus, E. coli, B. subtilis (MIC: 18.8, 9.4, 37.5, 9.4 μg/mL). Maximin 68 has hemolytic activities against human and rabbit red cells.