PFKFB3

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

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

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.

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

AZ-PFKFB3-67 is a novel potent and selective PFKFB3 inhibitor.

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

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.

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.

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.

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.

(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.