Activators & Inhibitors

Antifungal agent 33 (compound 4e) is a potent antifungal agent with significant antifungal activity against Candida albicans (MIC: 16 μg/ml). (IC50: 0.19 μg/ml).

Antitrypanosomal agent 4 (compound 19) is a potent antitrypanosomal agent that crosses the blood-brain barrier and shows good resistance to Trypanosoma cruzi and T. b. brucei with IC50 values of 1.2 μM and 70 nM respectively.

Anagliptin (SK-0403) hydrochloride is a potent, highly selective, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4) (IC50: 3.8 nM) with relatively weak selectivity for DPP-8 (IC50: 68 nM) and DDP-9 (IC50: 60 nM).

Tandospirone (SM-3997) hydrochloride is a potent, selective 5-HT1A receptor partial agonist (Ki: 27 nM) that exhibits anxiolytic and antidepressant activity. tandospirone hydrochloride can be used to study central nervous system disorders and their underlying mechanisms.

Influenza virus-IN-5 (Compound 5f) is an influenza virus hemagglutinin (HA) inhibitor that acts on the A/H3N2 virus (EC50: 1 nM).

Tubulin polymerization-IN-9 is a potent inhibitor of tubulin (IC50: 1.82 μM). Tubulin polymerization-IN-9 arrests the cell cycle of K562 cells in G2/M phase and induces apoptosis and mitochondrial depolarization. Tubulin polymerization-IN-9 exhibits potent anti-vascular and anti-tumour effects.

Parapenzolate bromide is an orally active mAChR antagonist. parapenzolate bromide is an anticholinergic and antitussive agent.

NN-390 is a selective, potent HDAC6 inhibitor (IC50: 9.8 μM) that crosses the blood-brain barrier. nN-390 has potential for studies in metastatic group 3 neural tube cell tumours.

DGAT1-IN-3 is a selective, potent, orally active DGAT-1 inhibitor that inhibits human DGAT-1 (IC50: 38 nM) and rat DGAT-1 (IC50: 120 nM).DGAT1-IN-3 can be used in studies of obesity, dyslipidemia and metabolic syndrome.