AP-III-a4 hydrochloride

Research use only, not for human use.

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.

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.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 esult:Inhibited cell migration dose-dependently.RT-PCR Cell Line:Huh7 and HEK Concentration:10 μM Incubation Time:24 hResult:Induced glucose uptake and inhibited PEPCK expression.

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.

ENOblock hydrochloride

Apoptosis

Apoptosis

IC50: 0.576 uM (enolase)

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2070014-95-6

631.18

C31H44ClFN8O3

>98% (HPLC)

In Vitro:?DMSO : ≥ 53 mg/mL (83.97 mM)

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(-20℃)

With Ice Pack

≥ 2 years