Selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor

Potent and Selective 5-Lipoxygenase Inhibitor

Novel Dipeptidyl peptidase IV (DPP-4) inhibitor, improving neovascularization by increasing both the number of circulating endothelial progenitor cells and endothelial nitric oxide synthetase expression

The class III antiarrhythmic agent, blocking HERG, a human cardiac delayed rectifier K+ channel

Novel potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R)

Potent and selective PDE4 inhibitor

Specific inhibitor of the cellular inosine-5-monophosphate dehydrogenase (IMPDH); Immunosuppressive agent

Antineoplastic DNA alkylating agent

Novel selective fluorescent H2O2 probe, tracking the mitochondria of live biological specimens and responds to local fluxes of hydrogen peroxide (H2O2) by a turn-on fluorescence enhancement

Novel potent antiproliferative mitochondria-targeted OXPHOS inhibitor (IC50=38 nM) in MiaPaCa-2 cells, being more effective than other inhibitors of OXPHOS in MiaPaCa-2 and U87MG cells

Novel mitochondrial-targeted pan-APT inhibitor

Radiation Mitigator, reducing lipid hydroperoxides and preventing apoptotic cell death

Fluorescent probe for measuring the activity levels of erasers of S-palmitoylation, acyl-protein thioesterases (APTs), within mitochondria of live cells

Sensitive and specific Raman probe for live cell imaging of mitochondria

The first small molecule inhibitor of Mitf-E-box DNA binding with depigmenting activity

Novel inhibitor of AMA1-RON2 interaction, blocking merozoite invasion from schizont-infected RBCs; Antidepressant; Acetylcholinesterase inhibitor

Novel degrader of Miro1 (mitochondrial Rho GTPase 1), reducing Miro1 levels in fibroblasts and stress-induced degeneration of dopaminergic neurons derived from Parkinson's disease (PD) patients, as well as age-dependent neuronal loss and prolongs lifespan

Novel Miro1 degrader, rescuing dopaminergic neurodegeneration and promoting Miro1 degradation in Parkinson’s Disease fibroblasts

Novel inhibitor of microRNA-21 (miR-21)

Novel specific and efficient inhibitor of miR-21 expression, inducing a 485% increase in the luciferase reporter signal at 10 μM

Novel thapsigargin-based PSMA-activated prodrug, inhibiting the sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump protein

Novel selective positive allosteric modulator (PAM) at the M1 muscarinic acetylcholine receptor

Novel photoactivatable allosteric ligand for the M1 muscarinic acetylcholine receptor

Novel long-lasting myostatin inhibitor, significantly increasing muscle mass and hindlimb grip strength in Duchenne muscular dystrophic model mice

Novel inhibitor of the prostate-specific membrane antigen (PSMA)

Novel inhibitor of the prostate-specific membrane antigen (PSMA)

Inhibitor of cholecystokinin B receptors (CCK2)

First-in-class inhibitor of MYC-induced nuclear antigen (MINA53) with selectivity over NO66 and other JmjC oxygenases

Natural anti-tumor agent, demonstrating with tumor inhibitory efficacy comparable or even superior to the mainstay chemotherapeutics paclitaxel or fluorouracil

MAO-B inhibitor and glycine prodrug, being studied for treatment for the symptoms of Alzheimer's disease