5MPN

• CAT Number: I044378
• CAS Number: 47208-82-2
• Molecular Formula: C15H19N3O4
• Molecular Weight: 305.33
• Purity: ≥95%
• Synonyms: 5-[(8-methoxyquinolin-4-yl)amino]pentyl nitrate
• InChI: InChI=1S/C15H19N3O4/c1-21-14-7-5-6-12-13(8-10-17-15(12)14)16-9-3-2-4-11-22-18(19)20/h5-8,10H,2-4,9,11H2,1H3,(H,16,17)
• InChIKey: YBOILUNNGBGURC-UHFFFAOYSA-N
• SMILES: COC1=CC=CC2=C(C=CN=C21)NCCCCCO[N+](=O)[O-]

5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines[1].
5MPN (0~30 μM; 24 hours; H460 cells) inhibits the expression of PFKFB4[1].
5MPN (0~50 μM; 0~72 hours; H460 NSCLC cells) first reduces the intracellular concentration of F2,6BP, glycolysis and ATP, which in turn results in a reduction in cell proliferation[1].
5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) induces cells apoptosis[1].
5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) arrests cell cycle progression[1].
5MPN (0.1, 1 or 10 µM) significantly inhibits PFKFB4 activity. 5MPN (H460 cells) leads to a dose-dependent decrease in the intracellular F2,6BP concentration. 5MPN (0~30 μM; over 48 hours; H460, H1299, H441, H522 and A549 cells) makes a dose-dependent reduction in cells growth. 5MPN (0~30 μM; 24 hours; H460 cells) inhibits PFKFB4 expression causing the observed reduction in H460 cell proliferation. 5MPN causes a G1 arrest in LLC cells in vitro similar to H460 cells[1].
5MPN (120 mg/kg; p.o.) suppresses the growth of Lewis lung carcinomas (LLC) grown in syngeneic mice and H460 human lung adenocarcinoma xenografts grown in athymic mice without affecting body weight[1].
5MPN causes a reduction in Ki67-positive cells in the LLC xenografts suggesting that 5MPN may be reducing cell cycle progression in vivo[1].

Reference

[1]. Chesney J, et al. Targeting the sugar metabolism of tumors with a first-in-class 6-phosphofructo-2-kinase (PFKFB4) inhibitor. Oncotarget. 2015;6(20):18001-18011.
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