GLPBio

AP-III-a4 hydrochloride

Catalog No.: GC35371Purity:>98%Synonyms: ENOblock hydrochloride
COASDSData Sheet
AP-III-a4 hydrochloride is the first non-substrate analog inhibitor of enolase (IC50 = 0.576μM).

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AP-III-a4 hydrochloride
Cas No.: 2070014-95-6
10mM (in 1mL DMSO)In Stock
$244.00
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2mgIn Stock
$88.00
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5mgIn Stock
$176.00
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10mgIn Stock
$279.00
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25mgIn Stock
$490.00
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Description

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.

Protocol

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:
[1]. 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.

Chemical Properties

CAS No.
2070014-95-6
Synonyms
ENOblock hydrochloride
SMILES
FC1=CC=C(CNC2=NC(NCC3CCCCC3)=NC(NC4=CC=C(CC(NCCOCCOCCN)=O)C=C4)=N2)C=C1.Cl
Molecular Formula
C31H44ClFN8O3
Molecular Weight
631.18
Solubility
DMSO: ≥ 53 mg/mL (83.97 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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