glut4

GLUT4-IN-2 is a specific GLUT4 inhibitor that inhibits GLUT1 and GLUT4.GLUT4-IN-2 has antitumor activity, induces apoptosis and cell cycle arrest, and can be used for cancer research.

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

β-Aminopropionitrile (3-Aminopropionitrile) is a selective inhibitor of lysyl oxidase.

Karanjin is a flavonoid obtained from the seeds of the karanja tree.Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis.

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.

Fasentin (N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide) is an inhibitor of GluT1.

KL-11743 specifically blocks glucose metabolism, triggering an acute collapse in NADH pools and a striking accumulation of aspartate, indicating a dramatic shift toward oxidative phosphorylation in the mitochondria.

GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).

GLUT4 activator3 (Compound 13a) is an antidiabetic agent that targets GLUT4 translocation in skeletal muscle. It facilitates the translocation of glucose transporter 4 (GLUT4) within skeletal muscle cells and effectively reduces blood glucose levels in diabetic rats induced by STZ.

M617 acetate is a selective agonist of galanin receptor 1 (GAL1). M617 acetate acts through central GAL1, promotes GLUT4 expression, and enhances GLUT4 content in the cardiac muscle of type 2 diabetic rats. The Ki values are 0.23 and 5.71 nM for GAL1 and GAL2, respectively.

DCW-234, recognized as an ERbeta selective agonist, displays enhanced binding affinity for ERbeta over ERalpha, effectively promoting a strong, selective ERbeta/SRC1 interaction. Studies have demonstrated that DCW-234 can induce GLUT4 expression in CHO-K1 cells.

Antidiabetic agent 7 (Compound 5m) functions as a potent hyperglycemia inhibitor. It effectively stimulates GLUT4 translocation in skeletal muscle cells by activating the AMPK-dependent pathway. Additionally, this compound is capable of reducing blood glucose levels and exhibits favorable pharmacokinetic properties. Antidiabetic agent 7 is suitable for research related to antihyperglycemic treatments.

Rapaglutin A is a glucose transporter (GLUT) inhibitor. It acts as a pan-GLUT inhibitor for the class I isomers GLUT1, GLUT3, and GLUT4, with an IC50 of 12 nM. Additionally, Rapaglutin A inhibits the proliferation of A549 cells.

DS-1150b is an orally active GLUT4 activator. It exhibits the ability to activate GLUT4 transport, facilitating the translocation of GLUT4 to the cell membrane in skeletal muscle cells. In a Zucker obese rat model, DS-1150b demonstrated hypoglycemic effects and can be utilized for research in type 2 diabetes mellitus (T2DM).

JTT-553 is a DGAT1 inhibitor with an IC50 of 2.38 nM. It effectively reduces plasma levels of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and liver triglycerides (TG). JTT-553 enhances insulin-dependent glucose absorption and glucose intolerance in the adipose tissue of diet-induced obese (DIO) mice. In KK-Ay mice, it lowers TNF-α mRNA levels and elevates GLUT4 mRNA levels in adipose tissue. By contributing to weight loss, JTT-553 improves insulin resistance in adipose tissue and overall glucose metabolism. This compound is useful for research on obesity and type 2 diabetes mellitus (T2DM).

VSP-77 is an orally active PPARγ agonist. It selectively enhances the expression of insulin sensitivity-related genes (Glut4 and Adiponectin) by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. In a high-fat diet-induced diabetic mouse model, VSP-77 significantly improves glucose tolerance and reduces fasting blood glucose and insulin levels. VSP-77 is applicable for diabetes research.

GTPγS (Guanosine 5'-[γ-thio]triphosphate) acts as a G protein activator, protecting proteins from proteolytic degradation. It stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, enhances phospholipase activity, and induces actin polymerization. The combination of GTPγS and G protein α is useful for studying kinase activity. Additionally, GTPγS can be included as a component of lysis buffers.

HK2-IN-3 (compound 12) is a potent hexokinase 2 (HK2) inhibitor with an IC50 of 56.4 nM. It reduces glucose uptake and downregulates GLUT1/GLUT4 expression in oral squamous cell carcinoma (OSCC). HK2-IN-3 induces mitophagy (mitophagy) and apoptosis (apoptosis). In OSCC xenograft mouse models, HK2-IN-3 suppresses tumor growth and angiogenesis. It can be utilized in OSCC research.

Chromium chloride is a trivalent chromium compound and one of the sources of trace elements essential for the body. It enhances insulin-mediated GLUT4 translocation and glucose uptake, regulates glucose and lipid metabolism, and inhibits oxidative stress and the production of inflammatory factors (such as TNF-α). In addition, chromium chloride can reduce lipid deposits in blood vessels and lower serum cholesterol levels, and is commonly used in research related to type 2 diabetes, metabolic syndrome, and atherosclerosis.

Rhoifolin (Apigenin 7-O-neohesperidoside) is extracted from Turpinia arguya Seem dried leaves.

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019). MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice. References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019).

10-PAHSA is a newly identified endogenous lipid that belongs to a collection of branched fatty acid esters of hydroxy fatty acids (FAHFAs). It is a FAHFA in which palmitic acid is esterified to 10-hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. As other FAHFAs improve glucose tolerance, stimulate insulin secretion, and have anti-inflammatory effects, 10-PAHSA may be a bioactive lipid with roles in metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to either a C-16 or C-18 hydroxy substituent. 12-PAHSA is a FAHFA in which palmitic acid is esterified at the 12th carbon of hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. 12-PAHSA is present at 2- to 3-fold higher levels in adipose tissue of AG4OX mice compared to wild type mice. Levels of 12-PAHSA are also higher in fasted wild-type mice compared to fed mice and are reduced upon high-fat diet-induced obesity in insulin-resistant mice.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to a hydroxylated C-16 or C-18 lipid. 9-PAHSA is a FAHFA in which palmitic acid is esterified to 9-hydroxy stearic acid. PAHSAs are the most abundant forms of FAHFA in serum as well as white and brown adipose tissues of glucose tolerant AG4OX mice, which overexpress Glut4 specifically in adipose tissue. 9-PAHSA is the predominant isomer of PAHSA in wild type and AG4OX mice. It is found in humans and is reduced in the serum and adipose tissues of insulin-resistant humans. 9-PAHSA improves glucose tolerance, stimulates insulin secretion, and has anti-inflammatory effects in mice.