pfk

Kaempferitrin (Lespenephryl) has antidepressant-like effect related to the serotonergic system, principally 5-HT1A. Kaempferitrin exerts cytotoxic and antitumor effects against HeLa cells. Kaempferitrin stimulates glucose-metabolizing enzymes, promotes glucose homeostasis. Kaempferitrin exerts immunostimulatory effects on immune responses mediated by splenocytes, macrophages, PBMC and NK cells. Kaempferitrin induces cytotoxic effects to include: cell cycle arrest in G1 phase and apoptosis via the intrinsic pathway in a caspase-dependent pathway.

ML251 is a potent novel nanomolar inhibitor of T. brucei and T. cruzi phosphofructokinase[1]. ML251 inhibits T. brucei PFK (IC50=0.37 μM) and T. cruzi PFK (IC50=0.13 μM). ML251 can be used for the research of parasite[1].

PFK-IN-1 (compound 1) is an inhibitor of 6-phosphofructo-1-kinase (PFK), demonstrating IC50 values of 0.41 and 0.23 μM against T. brucei and T. cruzi PFK, respectively, and an ED50 of 15.18 μg/mL for T. brucei. The compound has a half-life of 9.7 minutes in rat liver microsomes and 408 minutes in mouse liver microsomes.

PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

PFK-158 is an effective and specific inhibitor PFKFB3.

AZ PFKFB3 26 is an effective and selective PFKFB3 inhibitor with an IC50 of 23 nM. The IC50s for PFKFB1 and PFKFB2 are 2.06 and 0.384 μM, respectively.

AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with an IC50=11nM for PFKFB3, reduces MCL-1, and inhibits angiogenesis by decreasing lactic acid production and ATP levels in endothelial cells (ECs) in tube-forming assays, and has neuroprotective effects.

AZ-PFKFB3-67 quarterhydrate is a selective and potent inhibitor of the metabolic kinase PFKFB3 kinase, acting on PFKFB3 (IC50: 11 nM), PFKFB2 (IC50: 159 nM) and PFKFB1 (IC50: 1130 nM).

PFKFB3-IN-2 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). Anti-sense treatment against PFKFB3 has demonstrated a reduction in tumor growth rate in vivo.