[CAS NO. 2070014-95-6] AP-III-a4hydrochloride
PRODUCTS SPECIFICATIONS [2070014-95-6]
DESCRIPTION [2070014-95-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 631.18 |
| Molecular Formula | C31H44ClFN8O3 |
| SMILES | FC1=CC=C(CNC2=NC(NCC3CCCCC3)=NC(NC4=CC=C(CC(NCCOCCOCCN)=O)C=C4)=N2)C=C1.Cl |
3 Publications Citing Use of MCE
Summary
IC50 & Target
IC 50 : 0.576 uM (enolase) [1]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| 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 [1]
| 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 [1]
| 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 [1]
| Cell Line: | HCT116 |
| Concentration: | 0.625, 1.25 and 2.5 μM |
| Incubation Time: | 24 h |
| Result: | Inhibited cell migration dose-dependently. |
RT-PCR [1]
| Cell Line: | Huh7 and HEK |
| Concentration: | 10 μM |
| Incubation Time: | 24 h |
| Result: | Induced glucose uptake and inhibited PEPCK expression. |
In Vivo
AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | The zebrafish cancer cell HCT116 xenograft model [1] |
| Dosage: | 10 μM |
| Administration: | 96 h |
| Result: | Reduced cancer cell dissemination. Inhibited PEPCK expression and induced glucose uptake. Inhibited adipogenesis and foam cell formation. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 53 mg/mL ( 83.97 mM )
H 2 O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5843 mL | 7.9217 mL | 15.8433 mL |
| 5 mM | 0.3169 mL | 1.5843 mL | 3.1687 mL |
| 10 mM | 0.1584 mL | 0.7922 mL | 1.5843 mL |