AP-III-a4

Research use only, not for human use.

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

AP-III-a4 is the first, nonsubstrate inhibitor of enolase, blocking cancer cell metastasis in vivo.

AP-III-a4 (ENOblock) (0-10 μM; 24 h) inhibits HCT116 cell viability in a dose-dependent manner.AP-III-a4 directly binds to enolase and inhibits its activity.AP-III-a4 (0-10 μM; 24 or 48 h) inhibits cancer cell migration and invasion, induces cancer cell apoptosis.AP-III-a4 (10 μM; 24 h) can induce glucose uptake and inhibit phosphoenolpyruvate carboxykinase (PEPCK) expression in hepatocytes and kidney cells.Cell Viability Assay Cell Line:HCT116 Concentration:1.25, 2.5, 5 and 10 μM Incubation Time:24 h Result:Induced higher levels of HCT116 colon cancer cell death in hypoxic conditions compared to normoxia.Western Blot Analysis Cell Line:HCT116 Concentration:1.25, 2.5, 5 and 10 μM Incubation Time:24 h for AKT, 48 h for Bcl-Xl Result:Bound to enolase in cell lysate and bound to purified enolase. Decreased the expression of AKT and Bcl-Xl, which are negative regulators of apoptosis.Cell Invasion Assay Cell Line:HCT116 Concentration:0.156, 0.312, 0.625, 1.25 and 2.5 μM Incubation Time:24 h Result:Significantly inhibits cancer cell invasion at a treatment concentration of 0.625 μM.Cell Migration Assay Cell Line:HCT116 Concentration:0.625, 1.25 and 2.5 μM Incubation Time:24 h Result:Inhibited cell migration dose-dependently.RT-PCR Cell Line:Huh7 and HEK Concentration:10 μM Incubation Time:24 h Result:Induced glucose uptake and inhibited PEPCK expression.

AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish. Animal Model:The zebrafish cancer cell HCT116 xenograft model Dosage:10 μM Administration:96 h Result:Reduced cancer cell dissemination. Inhibited PEPCK expression and induced glucose uptake. Inhibited adipogenesis and foam cell formation.

AP-III-a4

Metabolic Enzyme/Protease

FAAH

enolase

Cancer

——

1177827-73-4

631.18

C31H44ClFN8O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (168.15 mM)

C1CCC(CC1)CNc1nc(nc(n1)NCc1ccc(cc1)F)Nc1ccc(cc1)CC(=O)NCCOCCOCCN

N-[2-[2-(2-Aminoethoxy)ethoxy]ethyl]-2-[4-[[4-(cyclohexylmethylamino)-6-[(4-fluorophenyl)methylamino]-1,3,5-triazin-2-yl]amino]phenyl]acetamide

(-20℃)

With Ice Pack

≥ 2 years