t 82

T 82 is an antagonist of 5-HT3 and inhibitor of acetylcholinesterase (AChE) and used for the treatment of Alzheimer's Disease.

T-82 is an acetylcholinesterase inhibitor that may ameliorate the impairment of memory induced by acetylcholinergic dysfunction.

Antibacterial agent 82 (compound 7p) exhibits antibacterial properties [1].

Anticancer agent 82 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin ( VIM ), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Anticancer agent 82 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 [1].

Antifungal agent 82 (compound G34) exhibits outstanding in vitro antifungal efficacy against Valsa mali, with an EC50 value of 0.57 μg/mL, and demonstrates excellent in vivo protective effects at 40 μg/mL [1].

OT-82 is a potent, selective, and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).

Lumacaftor (VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM).

FT827 is a covalent inhibitor of selective ubiquitin-specific protease 7 (USP7) (Ki=4.2 µM, Kd=7.8 µM) targeting the catalytic center of the autoinhibitory apolipoprotein form of USP7 for cancer research.

Metofenazate difumarate is a selective calmodulin inhibitor.

Antitumor Agent-82 is a potent anti-tumor compound that exhibits anti-proliferative activity and induces cell autophagy through the ATG5/ATG7 signaling pathway.

T-5342126 is a toll-like receptor 4 (TLR4) antagonist that reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50 = 27.8 μM) and decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s = 110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) also reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.

Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable thioethers as odorless products.2 1.Yamada, T., Iritani, M., Ohishi, H., et al.Pericosines, antitumour metabolites from the sea hare-derived fungus Periconia byssoides. Structures and biological activitiesOrg. Biomol. Chem.5(24)3979-3986(2007) 2.Du, L., Munteanu, C., King, J.B., et al.An electrophilic natural product provides a safe and robust odor neutralization approach to counteract malodorous organosulfur metabolites encountered in skunk sprayJ. Nat. Prod.82(7)1989-1999(2019)

AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226/S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T/C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.

Antitumor agent-172 (Compound 28) acts as an inhibitor of the β-catenin/BCL9 interaction, featuring an IC50 of 3.92 μM. This compound exhibits high affinity for β-catenin, with a Kd of 82 nM. Furthermore, Antitumor agent-172 activates T cells, enhances antigen presentation, and demonstrates antitumor activity along with favorable pharmacokinetic properties in murine models.

C-Reactive Protein (CRP) 77-82 is the 77-82 fragment of C-Reactive Protein. CRP, the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis. CRP is an annular (ring-shaped), pentameric protein found in blood plasma, whose circulating concentrations rise in response to inflammation. It is an acute-phase protein of hepatic origin that increases following interleukin-6 secretion by macrophages and T cells.

C-Reactive Protein (CRP) 77-82 acetate is the 77-82 fragment of C-Reactive Protein. C-Reactive Protein (CRP), the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis.C-reactive protein (CRP) is an annular (ring