hexokinase 选择性抑制剂 | 激活剂 | 调节剂

Nodakenetin

Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.

1-Deoxynojirimycin

1-Deoxynojirimycin (duvoglustat, moranolin) is a potent α-glucosidase inhibitor and most commonly found in mulberry leaves. It has therapeutic potency against diabetes mellitus.

Dorzagliatin

Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a dual-acting glucokinase (GK) activator that improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes.

LY2608204

LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.

AM2394

AM-2394 is a structurally distinct glucokinase activator (GKA), activates glucokinase (GK) with an EC50 of 60 nM.

Butyl isobutyl phthalate 

Butyl isobutyl phthalate (BIP), isolated from the rhizoid of Laminaria japonica, is a non-competitive inhibitor of α-glucosidase with IC50 of 38 μM. Butyl isobutyl phthalate displays a significant hypoglycemic effect and has the potential for diabetes treatment.