pfk

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.

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.

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.

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.

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.

GSK 366 is a potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 values of 0.7 nM for P. fluorescens-KMO and 2.3 nM for human KMO.

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

LysRs-IN-2 is a lysine tRNA synthetase (KRS) inhibitor with antiparasitic activity that inhibits Plasmodium falciparum KRS (PfKRS) and Cryptosporidium minum KRS (CpKRS), and is used in the study of malaria infections.

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration

Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, acting as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM[1].

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

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.

Stibophen is a potent antiparasitic agent effective against Litomosoides carinii, Dipetalonema witei, and Brugia pahangi. It inhibits lactate accumulation and phosphofructokinase (PFK) activity in adult filarial worms. Additionally, Stibophen suppresses PFK activity in Ascaris and Hymenolepis diminuta, without affecting mammalian liver PFK. It is utilized in studies of schistosomiasis and filarial infections.