Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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Targets |
IC50: 0.576 uM (enolase)[1]
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ln Vitro |
In a dose-dependent manner, AP-III-a4 hydrochloride (ENOblock) (0-10 μM; 24 h) decreases the viability of HCT116 cells [1]. Enolase's activity is inhibited by AP-III-a4 hydrochloride, which binds to it directly [1]. AP-III-a4 hydrochloride (0–10 μM; 24 or 48 h) causes cancer cells to undergo apoptosis and inhibits their migration and invasion [1]. AP-III-a4 hydrochloride (10 μM; 24 h) suppresses the production of phosphoenolpyruvate carboxykinase (PEPCK) and promotes hepatocytes and renal cells to ingest glucose [1].
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ln Vivo |
In zebrafish, AP-III-a4 hydrochloride (ENOblock) (10 μM; 96 h) suppresses the spread of cancer cells and the gluconeogenesis regulator PEPCK[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: HCT116 Tested Concentrations: 1.25, 2.5, 5 and 10 μM Incubation Duration: 24 h Experimental Results: Induced higher levels of HCT116 colon cancer cell death in hypoxic conditions compared to normoxia. Western Blot Analysis[1] Cell Types: HCT116 Tested Concentrations: 1.25, 2.5, 5 and 10 μM Incubation Duration: 24 h for AKT, 48 h for Bcl-Xl Experimental Results: Bound to enolase in cell lysate and bound to purified enolase. diminished the expression of AKT and Bcl-Xl, which are negative regulators of apoptosis. Cell Invasion Assay[1] Cell Types: HCT116 Tested Concentrations: 0.156, 0.312, 0.625, 1.25 and 2.5 μM Incubation Duration: 24 h Experimental Results: Dramatically inhibits cancer cell invasion at a treatment concentration of 0.625 μM. Cell Migration Assay [1] Cell Types: HCT116 Tested Concentrations: 0.625, 1.25 and 2.5 μM Incubation Duration: 24 h Experimental Results: Inhibited cell migration dose-dependently. RT-PCR[1] Cell Types: Huh7 and HEK Tested Concentrations: 10 μM Incubation Duration: 24 h Experimental Results: Induced glucose uptake and inhibited PEPCK expression. |
Animal Protocol |
Animal/Disease Models: The zebrafish cancer cell HCT116 xenograft model[1]
Doses: 10 μM Route of Administration: 96 h Experimental Results: diminished cancer cell dissemination. Inhibited PEPCK expression and induced glucose uptake. Inhibited adipogenesis and foam cell formation. |
References |
[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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Molecular Formula |
C31H44CLFN8O3
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Molecular Weight |
631.18
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CAS # |
2070014-95-6
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Related CAS # |
AP-III-a4;1177827-73-4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1CCC(CNC2=NC(=NC(NC3=CC=C(C=C3)CC(NCCOCCOCCN)=O)=N2)NCC2C=CC(F)=CC=2)CC1.Cl
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 53 mg/mL (83.97 mM)
H2O : < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.