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5MPN

Catalog No. T40565 CAS 47208-82-2

5MPN is a novel compound that functions as a highly potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4). This compound demonstrates oral activity and serves as a first-in-class inhibitor. Through competitive inhibition of the F6P binding site, 5MPN effectively hinders the functionality of PFKFB4, with a Ki value of 8.6 μM. Importantly, it exhibits no inhibitory effects on PFK-1 or PFKFB3. By specifically targeting the sugar metabolism of tumors, 5MPN exerts its anti-proliferative effects on various human cancer cell lines.

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5MPN, CAS 47208-82-2

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Biological Description

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Description	5MPN is a novel compound that functions as a highly potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4). This compound demonstrates oral activity and serves as a first-in-class inhibitor. Through competitive inhibition of the F6P binding site, 5MPN effectively hinders the functionality of PFKFB4, with a Ki value of 8.6 μM. Importantly, it exhibits no inhibitory effects on PFK-1 or PFKFB3. By specifically targeting the sugar metabolism of tumors, 5MPN exerts its anti-proliferative effects on various human cancer cell lines.
Targets&IC50	PFKFB4:8.6 μM (KI)
In vitro	5MPN, ranging from 0 to 30 μM over 24 hours, suppresses PFKFB4 expression in H460 cells, and at concentrations of 0 to 50 μM from 0 to 72 hours, firstly diminishes F2,6BP levels, glycolysis, and ATP production in H460 NSCLC cells, consequently inhibiting cell proliferation. Moreover, 5MPN at 0 and 10 μM for 6 to 24 hours both triggers apoptosis and halts cell cycle progression in H460 cells. At doses of 0.1, 1, or 10 μM, it significantly reduces PFKFB4 activity and lowers F2,6BP concentrations in a dose-responsive manner. Similarly, application of 5MPN from 0 to 30 μM over 48 hours across various cell lines (H460, H1299, H441, H522, and A549) results in a dose-dependent suppression of cell growth. Notably, 5MPN also leads to G1 arrest in LLC cells in vitro, akin to its effect on H460 cells. Western Blot Analysis and Cell Proliferation Assays in H460 cells exhibit inhibited PFKFB4 expression and reduced cell proliferation at 0~30 μΜ and 0~50 μM, respectively, over 24 hours and 0~72 hours. Apoptosis and Cell Cycle Analysis indicate induced apoptosis and cell cycle arrest at concentrations of 0 and 10 μM over intervals of 6, 12, and 24 hours.
In vivo	5MPN (120 mg/kg; p.o.) effectively inhibits the growth of Lewis lung carcinomas (LLC) in C57BL/6 mice and H460 human lung adenocarcinoma xenografts in athymic mice, without impacting the animals' body weight. Additionally, a decline in the number of Ki67-positive cells within LLC xenografts indicates that 5MPN potentially interferes with cell cycle progression in vivo[1]. This was achieved through oral administration at a dosage of 120 mg/kg.

Molecular Weight	305.334
Formula	C15H19N3O4
CAS No.	47208-82-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

5MPN 47208-82-2 inhibitor inhibit

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