glucokinase

Glucokinase activator 1 is a liver-directed glucokinase activator [EC50: 34 nM].

Glucokinase is a biochemical reagent used as a biomaterial or organic compound for research in the life sciences.

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.

ARRY-403 is a novel glucokinase activator that reduces fasting and postprandial blood glucose in patients with type 2 diabetes.

Globalagliatin (LY2608204) has been used in trials studying the treatment of Diabetes Mellitus, Type 2.

WAY-297848 is a novel glucokinase activator for the prevention or treatment of hyperglycemia, diabetes mellitus, obesity, dyslipidemia, and metabolic syndrome.

AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM).

MK-0941 free base is an orally active glucokinase activator with potent glucose-lowering activity, making it a potential therapeutic agent for type 2 diabetes.

Dorzagliatin (HMS5552) is a dual-acting glucokinase (GK) activator. It also improves glycaemic control and pancreatic β-cell function in type 2 diabetes.

PF-04991532 is an effective, hepatoselective glucokinase activator. It has EC50s of 80 and 100 nM in human and rat, respectively.

Palmitelaidic Acid (trans-Palmitoleic acid) is one of the most abundant fatty acids in serum and tissue.

Glucokinase activator8 is an activator of glucose kinase (glucokinase).

Glucokinase activator7 is an activator of glucose kinase (Glucokinase) and can be utilized in research on diabetes and hyperglycemia [refer to compound on page 176].

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.

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.

Glucokinase Activator 3, a highly potent and complete activator of Glucokinase (GK), exhibits an AC50 value of 38 nM. This compound holds potential for type 2 diabetes research applications.

ADP-specific glucokinase, expressed in thermophilic archaea, is an ADP-specific enzyme that catalyzes the conversion of glucose to glucose-6-phosphate, thereby facilitating glycolysis. This enzyme can activate T cells and enhance the phagocytic activity of macrophages. It is used in research related to metabolic disorders, neurological diseases, and tumors.

D-(-)-3-Phosphoglyceric acid disodium (3-Phospho-D-glyceric acid disodium) is an intermediate in glycolysis/gluconeogenesis and the biosynthesis of serine, glycine, and threonine, competitively inhibiting yeast enolase. It also functions as an intermediate in biosynthetic pathways in plants, eukaryotes, and prokaryotes.

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.

KDM4-IN-2 is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.

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.

Oxfendazole (RS-8858), a broad spectrum benzimidazole anthelmintic, protects livestock against roundworm, strongyles and pinworms.

Gcase activator 2 is a β-glucocerebrosidase activator that induces dimerization of GCase at the endoplasmic reticulum (ER) and lysosomal pHs, increases lysosomal substrate metabolism, and has therapeutic potential for the treatment of Parkinson's and Gosheimer's diseases.

PSN-GK1 is a potent activator of glucokinase (EC50: 0.13 μM).