AP-III-a4 hydrochloride (Synonyms: ENOblock hydrochloride) |
| رقم الكتالوجGC35371 |
AP-III-a4 (ENOblock) هيدروكلوريد هو مثبط إنولياز تناظري غير ركيزة مع IC50 من 0.576 ميكرومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2070014-95-6
Sample solution is provided at 25 µL, 10mM.
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AP-III-a4 hydrochloride is the first non-substrate analog inhibitor of enolase (IC50 = 0.576μM) [1]. AP-III-a4 hydrochloride induces cell death under hypoxia and inhibits cancer cell migration and invasion by downregulating AKT and Bcl-xL expression [1]. AP-III-a4 hydrochloride is often used in cancer research [2-3].
In HCT116 cells, AP-III-a4 hydrochloride (10μM, 24h) induced cell death under hypoxia and inhibited cancer cell migration and invasion by downregulating AKT and Bcl-xL expressions [1]. In NCI-H929 cells, AP-III-a4 hydrochloride (0.2-1.6μM; 72h) inhibits the proliferation of cancer cells [4]. In H9c2 cells, AP-III-a4 hydrochloride (10μM, 24h) inhibitor group displayed markedly reduced glucose and lactate levels [5].
In the Multiple myeloma (MM) xenograft model, the combination of AP-III-a4 hydrochloride (10mg/kg; ip; 15d) and BTZ has a more significant growth inhibitory effect in vivo than AP-III-a4 hydrochloride or BTZ alone [4].
References:
[1]. Jung DW, Kim WH, Park SH, et al. A unique small molecule inhibitor of enolase clarifies its role in fundamental biological processes. ACS chemical biology. 2013 Jun 21; 8(6): 1271-1282.
[2]. Chen X, Xu H, Wu N, et al. Interaction between granulin A and enolase 1 attenuates the migration and invasion of human hepatoma cells. Oncotarget. 2017 Mar 17; 8(18): 30305.
[3]. Wang C, Huang M, Lin Y, et al. ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy. Nature Metabolism. 2023 Oct; 5(10): 1765-1786.
[4]. Gao X, Feng Q, Zhang Q, et al. Targeting enolase 1 reverses bortezomib resistance in multiple myeloma through YWHAZ/Parkin axis. Journal of Biomedical Science. 2025 Jan 20; 32(1): 9.
[5]. Guo Z, Liu S, Hou X, et al. Isorhamnetin Attenuates Isoproterenol-Induced Myocardial Injury by Reducing ENO1 (Alpha-Enolase) in Cardiomyocytes. Antioxidants. 2025 May 11; 14(5): 579.
| Cell experiment [1]: | |
Cell lines | NCI-H929 cells |
Preparation Method | NCI-H929 cells were cultured in RPMI-1640 or Dulbecco's modified Eagle's medium at 37℃ in a humidified atmosphere with 5% CO2. NCI-H929 cells were treated with 0.2-1.6μM AP-III-a4 hydrochloride for 72 hours. |
Reaction Conditions | 0.2-1.6μM; 72h |
Applications | AP-III-a4 hydrochloride inhibits the proliferation of cancer cells. |
| Animal experiment [1]: | |
Animal models | Multiple myeloma (MM) xenograft model |
Preparation Method | BALB/c nude mice were used for the xenograft experiments. The mice were randomly assigned to four groups: vehicle control group, bortezomib (BTZ) treatment group (1mg/kg), ENO1 inhibitor (AP-III-a4 hydrochloride) treatment group (10mg/kg), and combination treatment group (BTZ + AP-III-a4). AP-III-a4 and BTZ were administered via intraperitoneal injection every two days. Tumor volume and body weight were monitored regularly throughout the treatment period. |
Dosage form | 10mg/kg; ip; 15d |
Applications | In MM xenograft model, the combination of AP-III-a4 hydrochloride and BTZ has a more significant growth inhibitory effect in vivo than AP-III-a4 hydrochloride or BTZ alone. |
References: | |
| Cas No. | 2070014-95-6 | SDF | |
| المرادفات | ENOblock hydrochloride | ||
| Canonical SMILES | FC1=CC=C(CNC2=NC(NCC3CCCCC3)=NC(NC4=CC=C(CC(NCCOCCOCCN)=O)C=C4)=N2)C=C1.Cl | ||
| Formula | C31H44ClFN8O3 | M.Wt | 631.18 |
| الذوبان | DMSO: ≥ 53 mg/mL (83.97 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5843 mL | 7.9217 mL | 15.8433 mL |
| 5 mM | 316.9 μL | 1.5843 mL | 3.1687 mL |
| 10 mM | 158.4 μL | 792.2 μL | 1.5843 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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