A small molecule enolase inhibitor
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AP-III-a4

Item No. 19933

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[2-(2-aminoethoxy)ethoxy]ethyl]-4-[[4-[(cyclohexylmethyl)amino]-6-[[(4-fluorophenyl)methyl]amino]-1,3,5-triazin-2-yl]amino]-benzeneacetamide
CAS Number
1177827-73-4
Synonyms
  • ENOblock
Molecular Formula
C31H43FN8O3
Formula Weight
594.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
211, 268 nm
SMILES
FC(C=C1)=CC=C1CNC2=NC(NC3=CC=C(CC(NCCOCCOCCN)=O)C=C3)=NC(NCC4CCCCC4)=N2
InChi Code
InChI=1S/C31H43FN8O3/c32-26-10-6-25(7-11-26)22-36-30-38-29(35-21-24-4-2-1-3-5-24)39-31(40-30)37-27-12-8-23(9-13-27)20-28(41)34-15-17-43-19-18-42-16-14-33/h6-13,24H,1-5,14-22,33H2,(H,34,41)(H3,35,36,37,38,39,40)
InChi Key
MOVYITHKOHMLHC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    AP-III-a4 is a small molecule enolase inhibitor (IC50 = 0.576 µM) that inhibited cancer cell metastasis in an in vivo zebrafish cancer cell xenograft model.1 It also reduced hyperglycemia and hyperlipidemia in C57BL/Ksj-db/db mice, a transgenic model of type 2 diabetes.2 Another study found that AP-III-a4 did not directly block enolase activity in vitro and suggested the mechanism is indirect.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jung, D.-W., Kim, W.-H., Park, S.-H., et al. A unique small molecule inhibitor of enolase clarifies its role in fundamental biological processes. ACS Chem Biol. 8(6), 1271-1282 (2013).

    2. Cho, H., Um, J., Lee, J.-H., et al. ENOblock, a unique small molecule inhibitor of the non-glycolytic functions of enolase, alleviates the symptoms of type 2 diabetes. Sci. Rep. 7, 44186 (2017).

    3. Satani, N., Lin, Y.-H., Hammoudi, N., et al. ENOblock does not inhibit the activity of the glycolytic enzyme enolase. PLoS One 11(12), e0168739 (2016).