1. Metabolic Enzyme/Protease
  2. Enolase
  3. AP-III-a4 hydrochloride

AP-III-a4 hydrochloride (Synonyms: ENOblock hydrochloride)

Cat. No.: HY-15858A Purity: >98.0%
Handling Instructions

ENOblock Hcl(AP-III-a4 Hcl) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.

For research use only. We do not sell to patients.

AP-III-a4 hydrochloride Chemical Structure

AP-III-a4 hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 400 In-stock
Estimated Time of Arrival: December 31
5 mg USD 288 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
25 mg USD 900 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AP-III-a4 hydrochloride:

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Description

ENOblock Hcl(AP-III-a4 Hcl) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo. IC50 value: 0.576 uM [1] Target: enolase Enolase is a component of the glycolysis pathway and a “moonlighting” protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule “ENOblock”, which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small molecule screening in a cancer cell assay to detect cytotoxic agents that function in hypoxic conditions, which has previously been shown to induce drug resistance. Further analysis revealed that ENOblock can inhibit cancer cell metastasis in vivo. Moreover, an unexpected role for enolase in glucose homeostasis was revealed by in vivo analysis. Thus, ENOblock is the first reported enolase inhibitor that is suitable for biological assays. This new chemical tool may also be suitable for further study as a cancer and diabetes drug candidate.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 53 mg/mL (83.97 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

631.18

Formula

C₃₁H₄₄ClFN₈O₃

SMILES

FC1=CC=C(CNC2=NC(NCC3CCCCC3)=NC(NC4=CC=C(CC(NCCOCCOCCN)=O)C=C4)=N2)C=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
AP-III-a4 hydrochloride
Cat. No.:
HY-15858A
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AP-III-a4 hydrochloride

Cat. No.: HY-15858A