glucose uptake inhibitor

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

SIRT6-IN-5(SIRT6 inhibitor 5) is a potent and selective SIRT6 inhibitor with an IC50 value of 34 μM.SIRT6-IN-5 is immunosuppressive and chemo-sensitizing, increases H3K9 acetylation and glucose uptake in cultured cells, and reduces T-cell proliferation.

PTP1B-IN-22 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor that inhibits glucose uptake in skeletal muscle L6 myotubes.

1. Stearic acid (Cetylacetic acid) can reduce metastatic tumor burden. 2. Stearic acid leads to dramatically reduced visceral fat likely by causing the apoptosis of preadipocytes. 3. Stearic acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. 4. Stearic acid is a potent phosphatase 1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes. 5. Stearic acid has the potential to increase dry matter intake and yields of milk and milk components, without affecting conversion of feed to milk, body condition score, or body weight.

AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2]. AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM.

(Rac)-Glutipyran is a broad-spectrum GLUT inhibitor targeting both GLUT1 and GLUT3. This compound inhibits glucose uptake and significantly impedes the growth of various cancer cells, particularly demonstrating substantial inhibition of PANC-1 cell growth (IC50=1.8 μM) and glucose uptake (IC50=0.13 μM).

LXQ-87 is an orally administered, non-competitive inhibitor of PTP1B with an IC50 of 1.061 μM, demonstrating hypoglycemic activity. It alleviates insulin resistance and enhances cellular glucose uptake, making it useful for type 2 diabetes research.

α-Amylase-IN-12 (Compound 5e) is an α-amylase inhibitor with an IC50 of 0.15 mM, functioning through a mixed inhibition mode. It exhibits an IC50 of 9.40 mM against α-glucosidase. This compound enhances glucose uptake in yeast cells and demonstrates significant anti-glycation activity at high concentrations. α-Amylase-IN-12 is applicable for diabetes research.

15-LOX-IN-2 (Compound 2a) is an orally active inhibitor of COX-2/15-LOX and a partial agonist of PPARγ. It exhibits anti-inflammatory activity by inhibiting levels of 20-HETE, IL-1β, and TNF-α in LPS-treated RAW 264.7 cells. Additionally, it significantly enhances glucose uptake without the presence of insulin and is applicable in metabolic disease research.

Rapaglutin E (RgE) is an inhibitor of glucose transport proteins (GLUT). It exhibits dose-dependent inhibition of [3H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC cells, with IC50 values of 8.9 nM, 3.1 nM, 35.5 nM, and 74.2 nM, respectively. Additionally, Rapaglutin E suppresses cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells.

Luseogliflozin, a potent and competitive inhibitor of sodium-dependent glucose cotransporter 2 (SGLT2), competitively inhibits human SGLT2-mediated glucose uptake with a Ki value of 1.10 nM.

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

Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive, and orally active pan-PTP (protein tyrosine phosphatases) inhibitor with insulin-mimicking effects and anti-diabetic properties. BMOV is a potent insulin sensitizer and has been shown to improve cardiac dysfunctions in diabetic models. BMOV inhibits HCPTPA, PTP1B, HPTPβ, and SHP2 with IC50s of 126 nM, 109 nM, 26 nM, and 201 nM, respectively [1][2].

AS1938909 is a SHIP2 inhibitor that works by increasing Akt phosphorylation, glucose consumption, and glucose uptake in L6 myotubes, specifically upregulating the GLUT1 gene.

6-Benzylthioinosine, a broad-spectrum metabolic inhibitor, inhibits glucose uptake, decreases glycolysis and ATP concentration with minimal changes in ROS and mitochondrial respiration.

AZD6482 (S-isomer) is a potent, selective, ATP-competitive PI3Kβ inhibitor (IC(50) 0.01 μm), which can inhibit insulin-induced in vitro glucose uptake by human adipocytes (IC(50) is 4.4 μm).

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.

SW157765 is a selective glucose transporter GLUT8 (SLC2A8) inhibitor, a prodrug of many compounds, that selectively inhibits the uptake of fluorescent 2-deoxyglucose (2DG) in SW157765-sensitive cells in a dose-dependent manner, and can be used for the study of lung cancer.

BMS309403 is a potent and selective inhibitor of adipocyte fatty acid binding protein aFABP. It improves endothelial function in apolipoprotein E-deficient mice and cultured human endothelial cells. It interacts with the fatty acid binding pocket inside the protein and competitively inhibits the binding of endogenous fatty acids.

PF-06761281 (Compound 4a) is a potent and partially selective sodium-coupled citrate transporter protein (NaCT SLC13A5) inhibitor with IC50 values of 0.51, 13.2, and 14.1 µM for NaCT, NaDC, and NaDC, respectively, and has the advantage of being orally active, reducing hepatic and renal uptake of citrate and plasma glucose concentration for metabolic diseases.

GSK-3β inhibitor 6 is a highly potent inhibitor of GSK-3β with an IC50 value of 24.4 μM, significantly enhancing hepatocyte glucose uptake (38%). This compound holds great potential for studying diseases such as diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder [1].

GSK-3β inhibitor 7 is a GSK-3β inhibitor (IC50: 5.25 μM) that acts by inserting into the ATP-binding pocket of GSK-3β and forming hydrogen bonds. It exhibits a high rate of glucose uptake by hepatocytes (83.5%) and can be used to study various diseases such as cancer, diabetes, inflammation, Alzheimer's disease, and bipolar disorder.

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg ml. Gliclazide (5 mg kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).

MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent. It also inhibits the human glucose transporter, demonstrating high potency with an IC50 of 2.6 μM in glucose uptake assays and an EC50 of 1.23±0.04 μM against the 3D7 strain of the malaria parasite [1].