Activators & Inhibitors

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

MAO-B-IN-7 is a potent and blood-brain barrier permeable MAO-B and AChE inhibitor. MAO-B-IN-7 exhibits IC50 s of 41 nM, 87 nM and 0.3 μM for human AChE, electric eel AChE and MAO-B, respectively. MAO-B-IN-7 effectively alleviates oxidative stress and neuroinflammatory damage.

Antibacterial agent 76 (compound 9) is a potent antibacterial agent.

This compound is a dual 5-HT1A/5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with additional inhibitory activity against PDE4B/PDE7A (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM). Its antidepressant-like effect surpasses that of the reference agent, escitalopram.

c-ABL-IN-4 is a potent inhibitor of c-Abl.

Antitubercular agent-29 (compound 6xa) is a potent drug resistant (DR) Mycobacterium tuberculosis (Mtb) inhibitor. Antitubercular agent-29 exhibits MIC of 0.03 μg/mL against drug-susceptible (DS)-Mtb strains, MIC of 0.03-0.06 μg/mL against DR-Mtb strains. Antitubercular has favourable selectivity (SI>40) against Vero cells.

TRPC5-IN-3 is a potent TRPC5 inhibitor (IC50= 10.75 nM).

Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor with IC50 of 0.12 mM. Chitin synthase inhibitor 1 potently inhibits drug-resistant fungi variants.

Chitinase-IN-4 (compound 8f) is a potent and selective inhibitor of OfChi-h with an IC50 value of 0.1 μM and good insecticidal activity.