Hexokinase Inhibitor

2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.

3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities.

Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (K_i: 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis.

ZSW is a hexokinase 2 (HK2) inhibitor with human HK2 IC₅₀ of 0.48 μM, human HK2 K_a of 252.00 μM, and selectivity over HK3 and GCK. ZSW binds directly to HK2, inhibits its enzymatic activity, modulates macrophage phenotypes through glycolysis inhibition, and inhibits NF-κB nuclear translocation by preventing IκBα phosphorylation and degradation. ZSW alleviates inflammatory bowel disease (IBD) and improves the intestinal inflammatory state of IBD mice. ZSW can be used for the research of inflammatory bowel disease.

Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma.

HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC₅₀ value of 0.79 μM and a K_d value of 0.41 μM. HK2-IN-4 blocks the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells. HK2-IN-4 induces the production of apoptosis (apoptosis) markers in cancer cells, including increased p-AMPK/AMPK ratio and Bax levels, as well as decreased Bcl2 levels. HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression. HK2-IN-4 can be used in research related to colorectal cancer and non-small cell lung cancer.

Benitrobenrazide (BNBZ) is the orally active inhibitor for hexokinase 2 with an IC₅₀ of 0.53 µM. Benitrobenrazide causes DNA damage, and exhibits antitumor effect.

D-Mannoheptulose is a 7-carbon keto sugar found in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation by hexokinase isoenzymes. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat. D-Mannoheptulose has various functions as anti-oxidants, anticancer effects and energy sources.

Hexokinase II VDAC binding domain peptide (Hxk2VBD peptide) is a cell-permeable hexokinase II VDAC binding domain. Hexokinase II VDAC binding domain peptide inhibits mitochondrial localization of hexokinase 2 (HXK2). Hexokinase II VDAC binding domain peptide inhibits neurotrophic factor-directed axon outgrowth.

2-Deoxy-D-glucose 6-phosphate disodium is an ATP-competitive, 2-deoxy-D-glucose non-competitive Hexokinase inhibitor, with a K_i value of 1.45 mM against bovine heart hexokinase. 2-Deoxy-D-glucose 6-phosphate disodium exerts ATP-competitive and 2-deoxy-D-glucose non-competitive inhibitory effects on bovine heart hexokinase. 2-DG inhibits glycolysis via the production and intracellular accumulation of 2-Deoxy-D-glucose 6-phosphate disodium, thereby inhibiting the functions of hexokinase and Glucose-6-phosphate isomerase, and inducing cell death. 2-Deoxy-D-glucose 6-phosphate disodium can be used in cancer-related research.

Licoflavone A is an orally active PTP1B/VEGFR-2 inhibitor, with an IC₅₀ of 54.5 μM against PTP1B, an IC₅₀ of 14.36 μM and a K_d of 142.38 nM against human VEGFR-2. Licoflavone A blocks the PI3K/AKT and MEK/ERK signaling pathways. Licoflavone A induces G1 phase cell cycle arrest, apoptosis via the intrinsic mitochondrial pathway (apoptosis), and inhibits migration, invasion and epithelial-mesenchymal transition (EMT) of gastric cancer cells. Licoflavone A inhibits the proliferation of gastric cancer cells in vitro and in xenograft models. Licoflavone A reduces the expression levels of HIF-1α, GLUT1, LDHA, PKM2 and HK2 in hypoxic gastric cancer cells, decreases glucose uptake and suppresses glycolysis. Licoflavone A can be used in research related to gastric cancer, type 2 diabetes and obesity.

HK-2-IN-1 is a Hexokinase 2 (HK-2) inhibitor. HK-2-IN-1 exhibits a non-activating effect on human recombinant HK-2 enzyme. HK-2-IN-1 has anti-tumor activity, affecting immune cells in the tumor microenvironment. HK-2-IN-1 has immunomodulatory effects and is potentially useful in the study of cancers such as colon cancer, liver cancer, and breast cancer.

Metrizamide (Amipaque) is used as the contrast medium for angiography in neuroradiological investigations. Metrizamide inhibits human brain hexokinase.

Lonidamine (Standard) is the analytical standard of Lonidamine. This product is intended for research and analytical applications. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (K_i: 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis.

HK2-IN-3 is a selective HK2 inhibitor with a human IC₅₀ of 0.0564 μM (56.4 nM). HK2-IN-3 induces mitophagy in oral squamous cell carcinoma cells. HK2-IN-3 exerts anti-cancer activity in oral squamous cell carcinoma cells. HK2-IN-3 can be used for the research of oral squamous cell carcinoma.

2-Deoxy-D-glucose 6-phosphate sodium is an ATP-competitive, 2-deoxy-D-glucose non-competitive Hexokinase inhibitor, with a K_i value of 1.45 mM against bovine heart hexokinase. 2-Deoxy-D-glucose 6-phosphate sodium exerts ATP-competitive and 2-deoxy-D-glucose non-competitive inhibitory effects on bovine heart hexokinase. 2-DG inhibits glycolysis via the production and intracellular accumulation of 2-Deoxy-D-glucose 6-phosphate sodium, thereby inhibiting the functions of hexokinase and Glucose-6-phosphate isomerase, and inducing cell death. 2-Deoxy-D-glucose 6-phosphate sodium can be used in cancer-related research.

HK2-IN-2 (Compound 26) is a Hexokinase 2 inhibitor that demonstrates significant anti-tumor activity by targeting microtubules and Hexokinase 2, with an IC₅₀ value of 0.764 μM against MD-MBA-231 cells. HK2-IN-2 effectively inhibits the activity of Hexokinase 2, leading to the accumulation of Reactive Oxygen Species and dysfunction of the mitochondrial membrane potential (MMP), thereby promoting apoptosis and blocking the cell cycle.

2-Deoxy-D-glucose 6-phosphate disodium is an ATP-competitive and 2-deoxy-D-glucose non-competitive Hexokinase inhibitor, with a K_i value of 1.45 mM against bovine heart hexokinase. 2-Deoxy-D-glucose 6-phosphate disodium exerts ATP-competitive and 2-deoxy-D-glucose non-competitive inhibitory effects on bovine heart hexokinase. 2-DG inhibits glycolysis via the generation and intracellular accumulation of 2-Deoxy-D-glucose 6-phosphate disodium, thereby inhibiting the functions of hexokinase and Glucose-6-phosphate isomerase, and inducing cell death. 2-Deoxy-D-glucose 6-phosphate disodium can be used in cancer-related research.

D-Mannoheptulose-¹³C is the ¹³C labeled D-Mannoheptulose (HY-U00462). D-Mannoheptulose is a 7-carbon keto sugar found in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation by hexokinase isoenzymes. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat. D-Mannoheptulose has various functions as anti-oxidants, anticancer effects and energy sources.

SID 24785302 is a hexokinase inhibitor with antiparasitic activity. SID 24785302 exhibits activity against T. brucei and Leishmania. SID 24785302 can be used for the research of mitochondrial DNA disorders and parasitic infection.