AP-III-a4 hydrochloride
(Synonyms: ENOblock hydrochloride) 目录号 : GC35371
AP-III-a4 hydrochloride是第一个非底物类似物烯醇化酶抑制剂（IC50 = 0.576μM）。
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.
AP-III-a4 hydrochloride是第一个非底物类似物烯醇化酶抑制剂（IC50 = 0.576μM） [1]。AP-III-a4 hydrochloride在缺氧条件下诱导细胞死亡，并通过下调AKT和Bcl-xL的表达来抑制癌细胞的迁移和侵袭 [1]。AP-III-a4盐酸盐常用于癌症研究 [2-3]。
在HCT116细胞中，AP-III-a4 hydrochloride（10μM，24h）在缺氧条件下诱导细胞死亡，并通过下调AKT和Bcl-xL的表达来抑制癌细胞的迁移和侵袭 [1]。在NCI-H929细胞中，AP-III-a4 hydrochloride（0.2-1.6μM；72h）抑制癌细胞的增殖 [4]。在H9c2细胞中，AP-III-a4 hydrochloride（10μM，24h）抑制剂组显著降低葡萄糖和乳酸水平 [5]。
在多发性骨髓瘤（MM）异种移植模型中，AP-III-a4 hydrochloride（10mg/kg；ip；15d）与BTZ联合用药比单独使用AP-III-a4盐酸盐或BTZ具有更显著的体内生长抑制作用 [4]。
| 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 | |
| 别名 | ENOblock hydrochloride | ||
| Canonical SMILES | FC1=CC=C(CNC2=NC(NCC3CCCCC3)=NC(NC4=CC=C(CC(NCCOCCOCCN)=O)C=C4)=N2)C=C1.Cl | ||
| 分子式 | C31H44ClFN8O3 | 分子量 | 631.18 |
| 溶解度 | DMSO: ≥ 53 mg/mL (83.97 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet