T6120

Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.

Antimalarial agent 3, an antimalarial agent, exhibits potent activity against Plasmodium with an IC50 of 0.035 μM. Furthermore, it demonstrates an exceptionally high selectivity index in relation to mammalian cells.

Ecopipam (SCH 39166) hydrochloride is a highly potent, selective, and orally active antagonist of dopamine D1/D5 receptors. It exhibits impressive binding affinities, with Ki values of 1.2 nM and 2.0 nM for D1 and D5 receptors, respectively. Ecopipam hydrochloride demonstrates remarkable selectivity, displaying over 40-fold selectivity compared to D2, D4, 5-HT, and α2a receptors, with Ki values of 0.98 μM, 5.52 μM, 0.08 μM, and 0.73 μM, respectively. Its application extends to various areas of research, including schizophrenia, cocaine addiction, and obesity [1] [3].

TDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), inhibiting indoleamine-2,3-dioxygenase, with antitumor activity that reverses local immune tolerance in tumor tissues.

ALK5-IN-8 is a highly effective inhibitor of TGFβRI (ALK5). It hinders the phosphorylation of ALK5 on downstream signaling proteins (Smad2 or Smad3) by obstructing the interaction between TGFβRI and ligands. Consequently, it disrupts or prevents TGF-β signaling. ALK5-IN-8 shows promise in the study of diverse diseases associated with ALK5-mediated pathways[1].

FPI-1465 is a dual inhibitor of serine-β-Lactamases and Penicillin-binding proteins (PBPs), demonstrating inhibition of PBP2 with an IC50 of 1.0 μg/mL. Additionally, it exhibits activity against β-lactamase CTX-M-15 and OXA-48, with dissociation constants (Kd) of 0.011 μM and 5.3 μM, respectively [1].

Nrf2/HO-1 activator 1 (Compound 24) is a potent neuroprotective and antioxidant agent targeting Nrf2/HO-1, with significant potential for therapeutic applications in Parkinson's disease (PD) research [1].

AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor that targets acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), with IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM against hAChE, hBChE, and hBACE-1, respectively. It exhibits significant binding affinity with PAS-AChE, excellent blood-brain barrier permeability, potential disassembly of amyloid-beta (Aβ) aggregates, neuroprotective properties against Aβ-induced stress, and remarkable antioxidant capabilities [1].

5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors, exhibiting K i values of 2 nM and 11 nM for the respective receptors, holding promise for research in neurological and psychiatric disorders [1].

PDE4-IN-11 is a potent phosphodiesterase isoenzyme 4 (PDE4) inhibitor, exhibiting remarkable bronchodilatory and anti-inflammatory characteristics. It is specifically designed for studying obstructive or inflammatory airway diseases [1] [2] [3].

HDAC-IN-27 is a highly potent and orally bioavailable class I HDAC-selective inhibitor with IC₅₀ values ranging from 0.43 to 3.01 nM against HDAC1–3. It shows significant anti-tumor activity in vitro and in vivo, exerts prominent anti-proliferative effects on acute myeloid leukemia (AML) cell lines, and achieves its biological effects by inducing apoptosis and promoting acetylation of histones H3 and H4 (AcHH3, AcHH4), making it applicable in acute myeloid leukemia research.