hek-4

AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.

GNE-0946 is a potent and selective agonist of RORγ, with an EC50 of 4 nM in HEK-293 cells.

Mt KARI-IN-4 (compound 5c) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki of 5.48 μM. It also inhibits Mtb H37Rv, displaying a minimum inhibitory concentration (MIC) of 0.78 μM, and exhibits low cytotoxicity, with an IC50 over 72 μg mL against human embryonic kidney cells (HEK) [1].

Apelin-36(human) TFA, an endogenous agonist of the orphan G protein-coupled receptor APJ, exhibits a potent EC50 of 20 nM and high affinity (pIC5 50 = 8.61) for human APJ receptors in HEK 293 cells. It is involved in significant cardiovascular and metabolic activities. Furthermore, Apelin-36(human) TFA can inhibit the entry of certain HIV-1 and HIV-2 strains into NP2/CD4 cells expressing the APJ receptor. [1] [2] [3] [4]