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Glucokinase

Glucokinase is an enzyme that facilitates phosphorylation of glucose to glucose-6-phosphate. Glucokinase occurs in cells in the liver and pancreas of humans and most other vertebrates. In each of these organs it plays an important role in the regulation of carbohydrate metabolism by acting as a glucose sensor, triggering shifts in metabolism or cell function in response to rising or falling levels of glucose, such as occur after a meal or when fasting. Mutations of the gene for this enzyme can cause unusual forms of diabetes or hypoglycemia.Glucokinase (GK) is a hexokinase isozyme, related homologously to at least three other hexokinases. All of the hexokinases can mediate phosphorylation of glucose to glucose-6-phosphate (G6P), which is the first step of both glycogen synthesis and glycolysis.

  • (E)-3PO
    T326013309-08-5
    (E)-3PO is a PFKFB3 (6-phosphofructo-2-kinase/fructose-2, 6-bisphosphatase) inhibitor.
    • $30
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    TargetMol | Citations Cited
  • MK-0941 free base
    T12056752240-01-0
    MK-0941 free base is an orally active glucokinase activator, exhibiting strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes.
    • $79
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  • (1S,2R)-Globalagliatin
    T3104L2514278-46-5In house
    (1S,2R)-Globalagliatin is a highly potent glucokinase (GK) activator for the study of type 2 diabetes.
    • $45
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  • ARRY-403
    T301421138669-65-4In house
    ARRY-403 is a novel glucokinase activator that reduces fasting and postprandial blood glucose in patients with type 2 diabetes.
    • $988
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  • WAY-640509
    T60048851185-20-1
    WAY-640509 is a glucocerebrosidase inhibitor.
    • $117
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  • AMG-1694
    T142121361217-07-3In house
    AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.
    • $380
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  • KDM4-IN-2
    T117492369607-62-3In house
    KDM4-IN-2 is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.
    • $1,520
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  • Globalagliatin
    T31041234703-40-2In house
    Globalagliatin (LY2608204) has been used in trials studying the treatment of Diabetes Mellitus, Type 2.
    • $32
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  • PF-04937319
    T164791245603-92-2In house
    PF-04937319 is an activator of glucokinase (EC50 =154.4  μM). PF-04937319 maintains glucose-lowering efficacy while mitigating the risk of hypoglycemia observed with many other glucokinase activators. PF-04937319 can be used in research on the treatment of type 2 diabetes mellitus.
    • $38
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  • AZ PFKFB3 26
    T143651704740-52-2In house
    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.
    • $30
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  • PFK-015
    T24554382-63-2
    PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).
    • $52
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    TargetMol | Citations Cited
  • PFK-158
    T31051462249-75-7
    PFK-158 is an effective and specific inhibitor PFKFB3.
    • $30
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    TargetMol | Citations Cited
  • PFKFB3-IN-2
    T67874794552-84-4
    PFKFB3-IN-2 is a 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) inhibitor. Anti-sense treatment against PFKFB3 was shown to reduce tumor growth rate in vivo.
    • $31
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  • SF2312
    T28764107729-45-3
    SF2312 is a natural phosphonate antibiotic produced by Actinobacillus microsporus and is a potent inhibitor of the glycolytic enzyme enolase.SF2312 has antimicrobial activity and inhibits bacterial growth against both Gram-negative and Gram-negative bacteria. SF2312 inhibits human recombinant ENO1 and ENO2.
    • $133
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  • Guajadial
    TN4174959860-49-2
    Guajadial shows α-glucosidase inhibitory activities significantly and its activity was better than that of Acarbose.Guajadial may act as Selective Estrogen Receptors Modulators (SERMs), therefore holding significant potential for anticancer therapy, it ex
    • $820
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  • Tuberosin
    TN519241347-45-9
    Tuberosin shows anti-inflammatory and antioxidant activities.It demonstrated a significantly potent inhibition on yeast α-glucosidase in a dose dependent manner.
    • $480
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  • WAY-297848
    T77784404360-27-6
    WAY-297848 is a novel glucokinase activator for the prevention or treatment of hyperglycemia, diabetes mellitus, obesity, dyslipidemia, and metabolic syndrome.
    • $30
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  • Tachioside
    TN5090109194-60-7
    Tachioside has antiobesity, antioxidant and α-glucosidase inhibitory activities, it decreases lipid content in 3T3-L1 adipocytes by inhibiting lipogenesis, shows antiobesity activities. Tachioside can inhibit nitric oxide production in lipopolysaccharides-stimulated RAW 264.7 cells with IC50 value of 12.14 μM.
    • $210
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  • Oxfendazole
    T071453716-50-0
    Oxfendazole (RS-8858), a broad spectrum benzimidazole anthelmintic, protects livestock against roundworm, strongyles and pinworms.
    • $30
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  • ML266
    T89901462267-08-8
    ML266, a glucocerebrosidase (GCase) chaperone with an IC50 of 2.5 µM, facilitates the transport of the mutant protein to the lysosome, thereby restoring GCase activity without inhibiting the enzyme's function. This compound shows promise for Gaucher disease research.
    • $48
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  • KAN0438757
    T117411451255-59-6
    KAN0438757 is a selective and potent inhibitor of the metabolic kinase PFKFB3 with an IC50 of 0.19 μM.
    • $103
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  • AMG-3969
    TQ00551361224-53-4
    AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM).
    • $123
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  • POMHEX
    T364912004714-34-3
    Pomhex, a cell-permeable potent enolase inhibitor with anticancer activity, is used in the study of cancer lethality.Pomhex, a racemic mixture, is a potent and selective ENO2 inhibitor.Pomhex is inhibitory to the glycolytic process, and shows anticancer activity at low concentrations in an ENO1-deficient tumor model.Pomhex, a cell-permeable potent enolase inhibitor with anticancer activity, is a potent and selective ENO2 inhibitor.
    • $148
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  • Palmitelaidic Acid
    T1950010030-73-6
    Palmitelaidic Acid (trans-Palmitoleic acid) is one of the most abundant fatty acids in serum and tissue.
    • $80
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  • Tangshenoside I
    TN5094117278-74-7
    Tangshenoside I might be a potential bioactive marker related to the hematopoietic and immunologic functions of Codonopsis Radix, which could be recommended as the index compound. It has α-glucosidase inhibition activity.
      7-10 days
      Inquiry
    • MitoPQ
      T334121821370-28-8
      MitoPQ (MitoParaquat) is a mitochondria-targeted small molecule compound that selectively enhances mitochondrial superoxide and hydrogen peroxide levels and inhibits insulin-stimulated glucose uptake and translocation of glucose transport protein 4 (GLUT4) to the plasma membrane in adipocytes and myotubes.MitoPQ can be used to MitoPQ can be used to study mitochondrial oxidative stress and regulated GLUT4 transporter.
      • $41
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    • PF-04991532
      T164801215197-37-7
      PF-04991532 is an effective, hepatoselective glucokinase activator. It has EC50s of 80 and 100 nM in human and rat, respectively.
      • $78
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    • AP-III-a4
      T67591177827-73-4
      AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.
      • $47
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    • ML198
      T89861380716-06-2
      ML198 is a novel activator and non-inhibitory chaperone of glucocerebrosidase. ML198 serves as a starting point to develop a novel approach towards small molecule treatment for patients suffering from Gaucher disease.
      • $40
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    • AZD-1656
      T26712919783-22-5
      AZD-1656 is a glucokinase activator (GKA) that can cause dose-limiting hypoglycemia in normal animals used in embryofetal development studies and type 2 diabetes.
      • $84
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    • YZ9
      T235526093-71-6
      PFKFB3 inhibitor
      • $50
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    • Genz-123346 free base
      T4049491833-30-8
      Genz 123346 is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1.
      • $43
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    • 3PO
      T2222318550-98-6
      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
      • $52
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    • ML251
      T643201486482-16-9
      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].
      • $135
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    • Pinoresinol diacetate
      TN479332971-25-8
      Pinoresinol diacetate inhibits the enzyme α-glucosidase in vitro and may therefore act as a hypoglycemic agent.
      • $460
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    • Cefetrizole
      T1075165307-12-2
      Ceftezole is an α-Glucosidase inhibitor (IC50: 2.1 μM; Ki: 0.578 μM).
      • $1,520
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    • AM-2394
      T33121442684-77-6
      AM-2394 is an effective and specific Glucokinase agonist (GKA, EC50: 60 nM), which catalyzes the phosphorylation of glucose to glucose-6-phosphate. AM-2394(AM2394) increases the affinity of GK for glucose by approximately 10-fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes.
      • $31
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    • Dorzagliatin
      T151591191995-00-2
      Dorzagliatin (HMS5552) is a dual-acting glucokinase (GK) activator. It also improves glycaemic control and pancreatic β-cell function in type 2 diabetes.
      • $34
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    • Cyclomusalenone
      TN374530452-60-9
      Cyclomusalenone is a potent α-glucosidase inhibitor.
      • $460
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    • 5MPN
      T4056547208-82-2
      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.
        7-10 days
        Inquiry
      • Kaempferitrin
        T3386482-38-2
        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.
        • $43
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