insulin-like

Insulin-like Growth Factor II (IGF-2), the primary somatomedin in human serum, exerts both permissive and direct influences on neurite outgrowth and significantly improves the survival of sympathetic and sensory neurons [1] [2].

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.

IGF-I (30-41) is a fragment of Insulin-like Growth Factor I (IGF-I) comprising amino acids 30 to 41.

IGF-I (24-41) is a 24-41 amino acid fragment of Insulin-like Growth Factor I (IGF-I), which contributes to systemic GH activities and exhibits various properties such as anabolic, antioxidant, anti-inflammatory, and cytoprotective.

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.

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

Indirubin Derivative E804 is a potent insulin-like growth factor type 1 receptor (IGF1R) inhibitor with potential antitumor activity.

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

D-Pinitol (Methylinositol) has anti-inflammatory activity. D-Pinitol(Methylinositol) exerts insulin-like activity, used for many diabetic associated conditions. D-Pinitol(Methylinositol) is a safe nutrient to reduce calorie consumption when supplementing with creatine.

Butanoic acid is an endogenous human metabolite, an endogenous histone deacetylase (HDAC) inhibitor. The IC50 of HDAC3, HDAC4 and HDAC1 were 2.4 mM, 4.5 mM and 5.3 mM, respectively. 3-Hydroxybutyric acid has the effects of energy metabolism, neuroprotection, anti-inflammatory, and improvement of insulin resistance.

Efpeglenatide is a long-acting agonist of the glucagon-like peptide-1 (GLP-1) receptor. Efpeglenatide improves insulin sensitivity, lowers blood glucose levels, and delays weight gain in diabetic and obese mouse models. Efpeglenatide has been applied in Type 2 diabetes research, providing an efficient experimental tool and preclinical evaluation value for developing metabolic disease intervention strategies, investigating weight loss mechanisms, and exploring insulin signaling regulation pathways.

ML-290 is an effective relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes. It shows an EC50 of 94 nM.

Semaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist. This compound mimics GLP-1 to lower blood glucose levels and stimulates the growth of pancreatic β-cells responsible for insulin production and release. Additionally, Semaglutide inhibits the production of glucagon, a hormone that enhances glycogenolysis [the release of liver-stored carbohydrates] and gluconeogenesis [the synthesis of new glucose]. By reducing appetite and slowing gastric emptying, it also helps decrease food intake and aids in reducing body fat.

KM04794 is a small molecule compound with chaperone-like functions that alleviates ER stress. This compound effectively prevents protein aggregation and cell death caused by ER stressors and mutant insulin proteins.

(2S,4R)-Teneligliptin is a selective inhibitor of dipeptidyl peptidase IV (DPP-4). It increases the concentration of active glucagon-like peptide-1 (GLP-1) in plasma, which in turn stimulates insulin secretion when blood glucose levels are elevated, thereby exhibiting hypoglycemic effects. (2S,4R)-Teneligliptin is a promising candidate for research in type 2 diabetes.

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.

GLP-1R modulator-1 (Compound 384) is a potent and orally active selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). It activates G protein-coupled signaling, leading to increased intracellular cAMP levels, enhanced insulin secretion, delayed gastric emptying, and reduced appetite. GLP-1R modulator-1 holds potential for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

GLP-1R agonist 34 (Compound 1) is an orally active small molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R). It enhances insulin secretion, suppresses glucagon release, and slows gastric emptying, thereby effectively reducing blood glucose levels. GLP-1R agonist 34 holds potential for research into metabolic disorders such as type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

NVP-DPP728 is a potent, reversible, nitrile-dependent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an inhibition constant (K i) of 11 nM for human DPP-IV amidolytic activity. By inhibiting the degradation of glucagon-like peptide-1 (GLP-1), NVP-DPP728 enhances insulin release following glucose intake, making it useful for diabetes research [1].

Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.

GSK2163632A is an insulin-like growth factor 1 receptor inhibitor that acts by binding to a novel region of the GRK active site cleft.

PF-06372222 is a small-molecule negative allosteric modulator of the glucagon receptor (GCGR). PF-06372222 is also an antagonist for glucagon-like peptide-1 receptor GLP-1R, which inhibits glucagon secretion and glucose-dependent insulin secretion.

AS1069562 is an inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake which acts by notably restoring reduced insulin-like growth factor 1 and fibroblast growth factor 2 mRNA levels in dorsal root ganglion and spinal cord, respectively.