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5MPN 

Cat. No.: HY-123981
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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 suppresses glucose metabolism and may yield favorable therapeutic indices suffering with advanced solid cancers.

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

5MPN Chemical Structure

5MPN Chemical Structure

CAS No. : 47208-82-2

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Description

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 suppresses glucose metabolism and may yield favorable therapeutic indices suffering with advanced solid cancers[1].

IC50 & Target

KI: 8.6 μM (PFKFB4)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: H460 cells
Concentration: 0~30 μΜ
Incubation Time: 24 hours
Result: Inhibited the expression of PFKFB4 .

Cell Proliferation Assay[1]

Cell Line: H460 NSCLC cells
Concentration: 0~50 μM
Incubation Time: 0~72 hours
Result: Resulted in a reduction in cell proliferation.

Apoptosis Analysis[1]

Cell Line: H460 cells
Concentration: 0 and 10 μΜ
Incubation Time: 6, 12 and 24 hours
Result: Induced cells apoptosis.

Cell Cycle Analysis[1]

Cell Line: H460 cells
Concentration: 0 and 10 μΜ
Incubation Time: 6, 12 and 24 hours
Result: Arrested cell cycle progression.
In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[1]
Dosage: 120 mg/kg
Administration: P.o.
Result: Suppressed 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.
Molecular Weight

305.33

Formula

C₁₅H₁₉N₃O₄

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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