T3979

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

LpxC-IN-5 is a potent, non-hydroxamate inhibitor of LpxC, which is an enzyme known as UDP-3-O-acyl-N-acetylglucosamine deacetylase. It exhibits an IC50 value of 20 nM. Furthermore, LpxC-IN-5 displays antibacterial activity against various strains including E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883, and P. aeruginosa 5567. The minimum inhibitory concentration (MIC) values for these strains are 16 μg/mL, 4 μg/mL, 64 μg/mL, and 4 μg/mL, respectively.

Mal-amide-PEG2-oxyamineBoc is a polyethylene glycol (PEG)-based linker molecule with a Boc-protected oxyamine functionality, serving as an efficient and versatile tool for the synthesis of PROTACs (proteolysis targeting chimeras).

AMPC is a TFF3 inhibitor with antitumor activity and inhibits tumor growth in vivo. AMPC inhibits cell proliferation and survival in TFF3-positive CMS4 colorectal cancer cells and can be used to study colorectal cancer.

Fmoc-Tyr(3-F, tBu)-OH is a cyclic peptide compound possessing high membrane permeability and exhibiting specific binding affinity towards a target molecule.

Bisabolone oxide A is a terpenoid isolated from Matricaria chamomilla L. It reduces neuronal excitability.Bisabolone oxide A inhibits α glucokinase and has been shown to inhibit α glucokinase in Helicoverpa armigera, Aedes vittatus, and Anopheles subpictus larvae and showed biotoxicity in Helicoverpa armigera, Aedes vittatus and Anopheles subpictus larvae experiments.

Tricarbonyldichlororuthenium(II) dimer (CORM-2) is a CO-releasing molecule with anti-inflammatory, antioxidant, and gastroprotective effects. It also modulates potassium channels independently of CO.

PDE12-IN-1 is a powerful and specific inhibitor of PDE12, exhibiting a pIC 50 value of 9.1 for enzyme inhibition. It effectively enhances levels of 2′,5′-linked adenylate polymers (2-5A), with a pEC 50 value of 7.7. Additionally, PDE12-IN-1 demonstrates antiviral activity.

RORγ agonist 1 is a highly potent and orally bioavailable compound that activates the RORγ receptor. Its efficacy is demonstrated by an EC50 value of 21 nM and it exhibits antitumor activity.

S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist used in the treatment of fibrotic diseases.

S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted with T-ALL cells.