T6179

Moxalactam sodium salt (LY-127935) is an antibiotic compound more effective against Escherichia coli and Pseudomonas aeruginosathan cephalosporins.

HIV-IN-6 is an HIV viral inhibitor that inhibits the replication of the HIV virus.HIV-IN-6 has anti-HIV viral activity and works by targeting Src family kinases (SFK) (e.g., Hck) that interact with the viral Nef protein.

AKR1C3-IN-6 (Compound 1) is a potent and specific AKR1C3 inhibitor, exhibiting IC50 values of 0.31 μM against AKR1C3 and 73.23 μM against AKR1C2. It demonstrates significant antitumor activity [1].

BRD4-BD1/2-IN-1 is a highly effective inhibitor of BRD4, targeting the BRD4 BD-1 and BD-2 domains with IC50 values of <100 nM each (US20150148375A1, compound 5) [1].

HDAC6-IN-10 is a potent and specific HDAC6 inhibitor, exhibiting an IC50 value of 0.73 nM. It demonstrates remarkable selectivity towards HDAC6, with a selectivity range of 144 to 10,941-fold over other HDAC isoforms. Furthermore, HDAC6-IN-10 exhibits notable anti-proliferative effects on multiple myeloma cells [1].

LASSBio-1632 is a novel anti-asthmatic lead candidate that selectively inhibits PDE4A and PDE4D isoenzymes, leading to the suppression of airway hyper-reactivity (AHR) and TNF-α production in lung tissue. With high experimental BBB permeability, LASSBio-1632 (7j) efficiently crosses the blood-brain barrier through passive diffusion [1].

BET-IN-9 is a BET inhibitor [1].

MtTMPK-IN-1 (compound 3) is a highly effective inhibitor of Mycobacterium tuberculosis thymidylate kinase (Mt TMPK), with an IC50 value of 2.5 μM. It shows moderate to weak activity against Mtb H37Rv and low cytotoxicity in human fibroblast cells MRC-5, making it a valuable tool for tuberculosis research [1].

HIV-1 inhibitor-15 (compound 9d) is a potent, broad-spectrum inhibitor targeting HIV-1, with EC50 values of 1.7 nM against HIV-1 WT, 4 nM against L100I, 2 nM against K103N, 6 nM against Y181C, and 9 nM against E138K. It exhibits high efficacy, favorable solubility, safety profiles, and oral bioavailability [1].

PARP-1-IN-1 is a highly selective and orally active inhibitor of the enzyme PARP-1 with an IC50 of 0.96 nM, exhibiting excellent tolerance and significant activity in a single dose in the MDA-MB-436 xenotransplantation model [1].

Antibacterial agent 75 (compound 24) exhibits antibacterial properties and notably re-sensitizes VRSA (Vancomycin-Resistant Staphylococcus aureus) strains to vancomycin, as reported in reference [1].