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AP-III-a4 hydrochloride
CAS No. 2070014-95-6
AP-III-a4 hydrochloride( ENOblock hydrochloride )
Catalog No. M25058 CAS No. 2070014-95-6
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.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
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Biological Information
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Product NameAP-III-a4 hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionAP-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.
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DescriptionAP-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.
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In VitroCell 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.
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In VivoAnimal 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.
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SynonymsENOblock hydrochloride
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PathwayApoptosis
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TargetApoptosis
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RecptorIC50: 0.576 uM (enolase)
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Research Area——
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Indication——
Chemical Information
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CAS Number2070014-95-6
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Formula Weight631.18
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Molecular FormulaC31H44ClFN8O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 53 mg/mL (83.97 mM)
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SMILES——
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
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 [Content Brief]
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