Novel quaternized GSK-3008348 derivative, acting as a highly selective αvβ6 Integrin Inhibitor

Novel potent RORγ inverse agonist

Potent and selective antagonist of P2X7 receptor

Novel selective inhibitor of G protein-coupled receptor kinase 2 (GRK2)

Promiscuous kinase inhibitor, a close analog of CTx-0294885

Novel agonist of toll-like receptor 2 (TLR2), stimulating the release of G-CSF in activated THP-1 cells, peripheral blood mononuclear cells, and human umbilical vein endothelial cells

Novel selective non-imidazole histamine H 3 receptor antagonist

Novel lysine specific histone demethylase 1 (LSD1) inhibitor, exhibiting high selectivity to LSD1 over MAOs

Novel inhibitor of prolyl hydroxylase (PHD) domain-containing enzyme

Novel anti-TB agent against Mycobacterium tuberculosis and Mycobacterium bovis BCG, targeting MmpL3 and inhibiting EchA6

Novel DNMT1-selective inhibitor (IC 50 = 0.11 ± 0.02 µM)

Novel highly potent cell-permeable, reversible, ATP-competitive inhibitor of GSK-3 (IC50 = 0.4 and 0.6 nM for GSK-3α and GSK-3β, respectively)

GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA.

Potent and irreversible inhibitor of GSK3

First-in-Class GSK-3β/HDAC Dual Inhibitor as a Disease-Modifying Agent To Combat Alzheimer’s Disease

Negative control for GSK4027

Novel specific inhibitor of polo-like kinase 1 (PLK-1), inducing cell death by causing cell cycle arrest at G2/M phase by competing with the ATP binding site of PLK-1 thus leading to apoptosis

Novel, Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitor

Novel selective inhibitor of G protein-coupled receptor kinase 2 (GRK2)

Novel highly potent and selective non-peptide oxytocin receptor antagonist

Novel potent EchA6 inhibitor

Novel inhibitor of the Ribonuclease H Activity of HIV-1 Reverse Transcriptase