Activators & Inhibitors

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.

HIV-1 inhibitor-31 (compound 4) is a potent inhibitor of HIV-1. HIV-1 inhibitor-31 can be used in the study of AIDS.

VEGFR-2-IN-16 (Compound 15b) is a potent inhibitor of VEGFR-2 (IC50: 86.36 nM) that exhibits antitumour effects.

HDAC-IN-47 is an orally active histone deacetylase (HDAC) inhibitor with IC50 values of 19.75 nM, 57.8 nM, 40.27 nM, 5.63 nM and 302.73 nM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. HDAC-IN-47 can block the cell cycle in G2/M phase, inhibit autophagy, induce apoptosis using the Bax/Bcl-2 and caspase-3 pathways, and has anti-cancer activity in vivo.