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.
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.
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