PFKFB3

PFKFB3 inhibitors act on a kinase that produces a key allosteric activator of glycolysis. 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) synthesizes fructose-2,6-bisphosphate, which in turn activates the glycolytic enzyme phosphofructokinase 1. Among the four family isoforms, PFKFB3 has the highest ratio of kinase to phosphatase activity. 3PO was reported in 2008 as a small molecule that lowers glycolytic flux by inhibiting PFKFB3. A 2013 study showed that PFKFB3-driven glycolysis controls vessel sprouting by endothelial cells. PFK15, its derivative PFK-158, KAN0438757 and AZ-PFKFB3-67 are other listed inhibitors. PFKFB4-IN-1 and 5MPN target the related isoform PFKFB4, which is also studied in tumor metabolism.

11 Items

  • 3PO
    Cat. No.
    A15932

    3PO

    3PO is a PFKFB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase) inhibitor.

    5 mg
    $45.00
    10 mg
    $65.00
    All 8 sizes
  • YZ9
    Cat. No.
    A13375

    YZ9

    YZ9 is a PFKFB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase) inhibitor with IC50 value of 0.183 μM.

    10 mg
    $40.00
    25 mg
    $75.00
    All 6 sizes
  • PFK15
    Cat. No.
    A14287

    PFK15

    Synonyms: PFK-015

    PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) with IC50 of 207 nM.

    5 mg
    $45.00
    10 mg
    $75.00
    All 8 sizes
  • PFK-158
    Cat. No.
    A14398

    PFK-158

    Synonyms: ACT-PEK-158

    PFK-158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) and derivative of 3-(3-pyridinyl)-1-[4-pyridinyl]-2-propen-1-one (3PO), with potential antineoplastic activity.

    1 mg
    $25.00
    2 mg
    $35.00
    All 8 sizes
  • KAN0438757
    Cat. No.
    A19216

    KAN0438757

    KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 0.19 μM .

    1 mg
    $95.00
    5 mg
    $195.00
    All 7 sizes
  • AZ PFKFB3 26
    Cat. No.
    A19281

    AZ PFKFB3 26

    AZ PFKFB3 26 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 23 nM. AZ PFKFB3 26 inhibits PFKFB1 and PFKFB2 with IC50s of 2.06 and 0.384 μM, respectively.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • PFKFB4-IN-1
    Cat. No.
    A25452

    PFKFB4-IN-1

    PFKFB4-IN-1 is a selective ATP-competitive inhibitor of PFKFB4, demonstrating an IC50 of 4.50 μM and over 12-fold selectivity against PFKFB1/4 and PFKFB3/4. This compound effectively reduces intracellular PFKFB4 protein levels and exhibits significant anti-cancer activities, including the inhibition of cell proliferation, induction of apoptosis, and suppression of cell migration. PFKFB4-IN-1 has shown efficacy in vivo, effectively inhibiting tumor growth in the MDA-MB-231 xenograft mouse model, making it a valuable tool for research in breast, lung, and liver cancer.

    5 mg
    $270.00
    10 mg
    $410.00
    All 3 sizes
  • 5MPN
    Cat. No.
    A36179

    5MPN

    5MPN is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4), exhibiting competitive inhibition at the fructose-6-phosphate binding site with a Ki of 8.6 μM. This compound does not affect PFK-1 or PFKFB3, allowing for targeted modulation of glucose metabolism in cancer cells. 5MPN has demonstrated the ability to suppress the proliferation of various human cancer cell lines, making it a valuable tool for research in cancer metabolism and therapeutic development.

    2 mg
    $80.00
    5 mg
    $140.00
    All 7 sizes
  • PFKFB3-IN-2
    Cat. No.
    A36252

    PFKFB3-IN-2

    PFKFB3-IN-2 is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). It demonstrates key biological activity by modulating glucose metabolism, making it relevant in cancer research and neurodegenerative disorders. This compound holds potential for applications in autoimmune diseases, inflammatory conditions, multiple sclerosis, metabolic disorders, and the study of angiogenesis.

    5 mg
    $35.00
    10 mg
    $55.00
    All 6 sizes
  • (E/Z)-3PO
    Cat. No.
    A36455

    (E/Z)-3PO

    (E/Z)-3PO is a selective inhibitor of PFKFB3, a key regulator of glycolysis. This compound effectively inhibits glycolysis, reduces the extracellular acidification rate, and suppresses angiogenesis by impairing endothelial cell migration and capillary tube formation. Research applications of (E/Z)-3PO include investigations into cancer, acute lung injury, pulmonary fibrosis, and atherosclerosis, making it a valuable tool for exploring therapeutic strategies in these diseases.

    1 mg
    $20.00
    5 mg
    $25.00
    All 6 sizes

11 Items

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