insulin-induced

Fatostatin hydrobromide (Fatostatin A HBr) ia an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.

Fatostatin is a specific inhibitor of SREBP activation, it impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

RH01386 is a small molecule that prevents ER stress-induced β cell dysfunction and death, inhibits proapoptotic gene expression, and restores ER stress-impaired glucose-stimulated insulin secretion responses, showing potential for type 2 diabetes treatment.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.

Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.

Oxfenicine (4-Hydroxy-L-phenylglycine) is a carnitine palmitoyltransferase-1 inhibitor. Oxfenicine improves whole-body glucose tolerance and insulin sensitivity in high-fat diet-induced obese mouse with insulin resistance.

Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties. It can increase glucose-induced insulin secretion and stimulate the electrical activity of α2-cells and enhance cytosolic Ca(2+) concentration ([Ca(2+)](c)).

CLT-28643 is a potent and specific α5β1-Integrin inhibitor that prevents fibrosis in glaucoma filtration surgery (GFS), inhibits tumor growth and angiogenesis, suppresses fibrosis and inflammation in a bleomycin-induced lung fibrosis model, and improves insulin sensitivity and cardiac function in H9C2 cells from obese mice.

Galantide acetate, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide acetate recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide acetate dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide acetate appears to bind to a single population of SP receptors (KD~40 nM).

D5D-IN-326 is an orally active delta-5 desaturase (D5D) inhibitor (IC50s: 72 and 22 nM for rat and human D5D in enzymic and cell-based assays). It has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in die

PPARγ agonist15 (Compound 7c) functions as an agonist of PPARγ, inhibiting the expression of α-amylase (HPA) and α-glucosidase (HLAG) with IC50 values of 28.35 µM and 26.21 µM, respectively. It enhances glucose uptake in L6 myotubes and improves glucose homeostasis, insulin sensitivity, and lipid metabolism in a rat model of Streptozotocin-induced diabetes.

Caspase-3-IN-3 (compound 7) is a caspase 3 inhibitor. It enhances cellular ATP levels, inhibits caspase-3 activity, reduces nitrite production, suppresses cytokine-induced apoptosis, and restores glucose-stimulated insulin secretion.

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).

ZP3022 is a dual agonist targeting the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor. It selectively enhances cAMP accumulation or ERK phosphorylation in HEK293 cells with GLP-1R or CCK2 receptor expression, compared to ERK phosphorylation in cells with the CCK1 receptor (EC50s: 0.02, 10.3, and >1,000 nM for human receptors, respectively). At 40 nM, ZP3022 promotes proliferation of rat neonatal β-cells in vitro. It also boosts glucose-induced insulin secretion (GSIS) in rat pancreatic islets at 10 and 100 nM concentrations and decreases body weight in rats at 40 nmol/kg doses twice daily. Administered at 100 nmol/kg daily, ZP3022 enhances β-cell and total pancreatic mass and improves glucose tolerance in db/db mice, while reducing food intake but not body weight in these mice.

MY17 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 0.41±0.05 μM. It alleviates insulin resistance induced by palmitic acid (PA) by enhancing the expression of phosphorylated insulin receptor substrate (IRS1) and protein kinase B (AKT). By binding to PTP1B, MY17 inhibits its activity, thereby improving insulin signaling and exhibiting antidiabetic properties. MY17 is useful in the study of type 2 diabetes.

PI3KC2γ-IN-1 (Compound 23) is an orally active and selective inhibitor of PI3KC2γ with an IC50 of 4 nM. It downregulates the Akt2-glycogen synthase (GS) signaling pathway, ultimately inhibiting the conversion of glucose to glycogen and reducing excessive glycogen accumulation in the liver. PI3KC2γ-IN-1 significantly inhibits insulin-induced accumulation of PI(3,4)P2 in primary hepatocytes and HepG2 liver cancer cells. It is useful for researching glycogen storage diseases (GSDs).

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.

CB1 antagonist6 (Compound 11jE2) is an orally active CB1R antagonist with an IC50 value of 23 nM. It significantly reduces food intake and body weight in diet-induced obesity (DIO) mice, improves glucose tolerance and insulin resistance, and lowers serum ALT and AST levels, demonstrating hepatoprotective effects. CB1 antagonist6 is applicable for studies on metabolic syndrome, including obesity and diabetes.

DRAK1/2-IN-2 (Compound Y17) is an inhibitor of DRAK1/2, with IC50 values of 353.2 nM for DRAK2 and 507.4 nM for DRAK1. This compound enhances mitochondrial membrane potential and glucose-stimulated insulin secretion (GSIS). It also combats lipotoxicity-induced apoptosis and significantly suppresses the secretion of the pro-inflammatory cytokine IL-1β, providing anti-inflammatory effects. Additionally, DRAK1/2-IN-2 significantly reduces blood glucose levels in mice and is applicable in diabetes research.

Efaroxan hydrochloride is the salt form of Efaroxan, a selective, orally available α2-adrenoceptor antagonist that raises resting plasma insulin levels and significantly potentiates adrenaline-induced increases in insulin levels.

HX 531 is a RXR antagonist (IC50 of 18 nM). HX 531 prevents HF diet-induced obesity, insulin resistance, and diabetes by reducing tissue TG content in white adipose tissue (WAT), skeletal muscle, and liver in mice.

AMG-221 is a potent and selective 11β-HSD1 inhibitor. AMG-221 decreased fed blood glucose and insulin levels and reduced body weight in diet-induced obesity mice.