JAK/STAT signaling

WZ-2-033 is a potent STAT3 inhibitor. It inhibits proliferation, colony survival, migration, and invasion of MDA-MB-231, HCC70, and MDA-MB231-4175 cells, with IC50 values of 0.7, 1.3, and 1.3 μM respectively.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and

KT621 Analog 2 also measured the DC50 value of STAT6 to be > 1 µM through the Meso Scale Discovery Assay (MSDA) method. This detection was derived after culturing the human cell line A549 at 37°C for 24 hours.

JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.