pfkfb4

5MPN is an orally active and selective inhibitor of 6-phosphofructokinase-2-kinase (PFKFB4) that competitively inhibits the F6P binding site and inhibits the proliferation of myeloma cells, and can be used in the study of myeloproliferative neoplasms.

PFKFB4-IN-1 is a potent and selective ATP-competitive inhibitor of PFKFB4 (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. It exhibits over 12-fold selectivity for PFKFB1/4 and PFKFB3/4 isoforms. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and suppresses cell migration. It also hinders tumor growth in MDA-MB-231 xenograft mouse models. PFKFB4-IN-1 is applicable for studies related to breast cancer, lung cancer, and liver cancer.