T8224

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

Halichondrin B, sourced from the sponge Halichondria okadai, serves as a noncompetitive inhibitor of Vinca-alkaloid binding to tubulin, with an IC 50 for tubulin polymerization ranging from 1.2-1.4 μM, and exhibits anti-tumor activity [1].

hAChE-IN-6 (compound 51) is a brain-penetrant acetylcholinesterase (AChE) inhibitor with an IC50 of 0.16 μM. It also inhibits human butyrylcholinesterase (hBuChE) and glycogen synthase kinase 3 beta (GSK3β), with IC50 values of 0.69 μM and 0.26 μM, respectively. Additionally, hAChE-IN-6 impedes the self-aggregation of tau protein and amyloid-beta 1-42 (Aβ1-42), making it useful for Alzheimer's disease (AD) research [1].

hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), showing IC50 values of 0.17 μM for both enzymes. It also potently inhibits glycogen synthase kinase 3 beta (GSK3β) with an IC50 of 0.21 μM. Furthermore, it effectively inhibits tau protein and Aβ1-42 peptide self-aggregation, and can bind the peripheral anionic site (PAS) to prevent amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) supports its potential in developing multitargeted anti-Alzheimer's agents [1].

Antitumor Agent-108 (Compound 5), an inhibitor of the Hyaluronic Acid (HA)-CD44 interaction, effectively disrupts cancer spheroid integrity and exhibits antiproliferative activity against cancer cells [1].

Gymnoside I (compound 1), a glycosidoxybenzyl 2-isobutylmalic acid, exhibits antiallergic properties, particularly in the passive cutaneous allergic reaction (PCA) test in mice. It holds potential for research applications in the treatment of asthma, neurasthenia, and chronic hepatitis [1].