AP-III-a4

• CAS: 1177827-73-4
• Catalog Number: ACM1177827734
• Category: Inhibitors
• Molecular Weight: 594.74
• Molecular Formula: C31H43FN8O3
• Description: AP-III-a4, also known as ENOblock, is the first, nonsubstrate inhibitor of enolase, blocking cancer cell metastasis in vivo. biochemical analysis showed that the half maximal inhibitory concentration (IC50) of enolase inhibition by ENOblock is 0.576 μM. ENOblock can inhibit cancer cell metastasis in vivo. Moreover, an unexpected role for enolase in glucose homeostasis was revealed by in vivo analysis. ENOblock is the first reported enolase; inhibitor that is suitable for biological assays.
• Synonyms: AP-III-a4; ENOblock
• IUPAC 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
• Canonical SMILES: O=C(NCCOCCOCCN)CC1=CC=C(NC2=NC(NCC3CCCCC3)=NC(NCC4=CC=C(F)C=C4)=N2)C=C1
• InChI: 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
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: ENOblock(AP-III-a4) 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.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 62.61; H, 7.29; F, 3.19; N, 18.84; O, 8.07
• Exact Mass: 594.3442
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: ENOblock was used to inhibit the activity of ENO1 in PAMC-82 and SNU16 cells and then investigated the changes of stemness in GCs. It was found that treatment with ENOblock (10 or 20 μM) could reduce the glycolysis level, that is, ENOblock could decrease glucose consumption and lactic acid production. Moreover, ENOblock treatment (10 or 20 μM) significantly decreased the ECAR levels of these cells. Furthermore, ENOblock treatment at 10 or 20 μM could significantly inhibit GCs' self-renewal capacity. The function of ENOblock on cell migration and invasion was then explored. The results indicated that treatment with ENOblock (10 or 20 μM) could strongly reduce cells' migration and invasion rates. Moreover, cells' cisplatin sensitivities were markedly increased by treatment with ENOblock at 10 or 20 μM. These results suggested that the function of inhibition by ENOblock was in consistent with the function of ENO1-knockdown.; Reference: Cell Death Dis. 2020 Oct 16;11(10):870. https://pubmed.ncbi.nlm.nih.gov/33067426/
• In Vivo Activity: TBD
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).