AP-III-a4 is a small molecule enolase inhibitor (IC50 = 0.576 µM) that inhibited cancer cell metastasis in an in vivo zebrafish cancer cell xenograft model. It also reduced hyperglycemia and hyperlipidemia in C57BL/Ksj-db/db mice, a transgenic model of type 2 diabetes. Another study found that AP-III-a4 did not...

Cell permeable first non-substrate analog enolase inhibitor (IC50=0.576µM). A recent study suggested no direct blocking of enolase activity in vitro and a indirect mechanism. Useful agent for immunometabolism research. The glycolysis enzymes enolase is known to have additional, non-glycolytic roles in cellular...

Description: AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 µM. Target: Glucokinase, Apoptosis. Smiles: NCCOCCOCCNC(=O)Cc1ccc(Nc2nc(NCC3CCCCC3)nc(NCc3ccc(F)cc3)n2)cc1. References: Jung DW, et al. ACS Chem Biol. 2013, 8(6), 1271-1282.