AP-III-a4 hydrochloride

• CAT Number: I046405
• CAS Number: 2070014-95-6
• Molecular Formula: C31H44ClFN8O3
• Molecular Weight: 631.18
• Purity: ≥95%
• Synonyms: N-[2-[2-(2-aminoethoxy)ethoxy]ethyl]-2-[4-[[4-(cyclohexylmethylamino)-6-[(4-fluorophenyl)methylamino]-1,3,5-triazin-2-yl]amino]phenyl]acetamide;hydrochloride
• InChI: InChI=1S/C31H43FN8O3.ClH/c32-26-10-6-25(7-11-26)22-36-30-38-29(35-21-24-4-2-1-3-5-24)39-31(40-30)37-27-12-8-23(9-13-27)20-28(41)34-15-17-43-19-18-42-16-14-33;/h6-13,24H,1-5,14-22,33H2,(H,34,41)(H3,35,36,37,38,39,40);1H
• InChIKey: UYGRNXLHKIBHMM-UHFFFAOYSA-N
• SMILES: C1CCC(CC1)CNC2=NC(=NC(=N2)NCC3=CC=C(C=C3)F)NC4=CC=C(C=C4)CC(=O)NCCOCCOCCN.Cl

AP-III-a4 (ENOblock) hydrochloride is a nonsubstrate analogue enolase inhibitor with an IC50 of 0.576 uM. AP-III-a4 hydrochloride can be used for the research of cancer and diabetic[1].
AP-III-a4 (ENOblock) (0-10 μM; 24 h) inhibits HCT116 cell viability in a dose-dependent manner[1].
AP-III-a4 directly binds to enolase and inhibits its activity[1].
AP-III-a4 (0-10 μM; 24 or 48 h) inhibits cancer cell migration and invasion, induces cancer cell apoptosis[1].
AP-III-a4 (10 μM; 24 h) can induce glucose uptake and inhibit phosphoenolpyruvate carboxykinase (PEPCK) expression in hepatocytes and kidney cells[1].
AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish[1].

Reference

[1]. Da-Woon Jung, et al. A Unique Small Molecule Inhibitor of Enolase Clarifies Its Role in Fundamental Biological Processes.ACS Chem. Biol., 2013, 8 (6), pp 1271–1282
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