igf-2

IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R), potentially reversing the transformed phenotype of tumor cells and increasing their susceptibility to apoptosis.

Pasireotide (SOM230) acetate is a long-acting cyclohexapeptide growth hormone inhibitory hormone analog with antisecretory, antiproliferative, and proapoptotic activities.Pasireotide (SOM230) acetate inhibits the secretion of GH, IGF-I, and ACTH, and can be used in the study of acromegaly and Cushing's disease. Pasireotide (SOM230) acetate also enhances the agonist activity of growth inhibitory receptors, with pKi of 8.2, 9.0, 9.1, <7.0 and 9.9 for sst1, 2, 3, 4 and 5, respectively.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.

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.

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

ALK inhibitor 1 is a selective ALK kinase inhibitor.

GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.

NVP-ADW742 (ADW) is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

NBI-31772 hydrate is a powerful inhibitor of the interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). It acts as a nonpeptide ligand, effectively releasing bioactive IGF-I from the IGF-I/IGFBP-3 complex (Ki values for all six human subtypes range from 1-24 nM). This compound demonstrates significant anxiolytic and antidepressant-like effects [1] [2] [3].

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].

Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, acts as a partial agonist at sst 2 sst 5 receptors, with IC50 values of 0.26 nM and 6.92 nM, respectively. It effectively inhibits the release of growth hormone and the production of insulin-like growth factor-1 (IGF-1), and either inhibits adenylate cyclase activity or promotes extracellular acidification. Angiopeptin TFA shows promise for use in coronary atherosclerosis research [1] [2].

Istiratumab (M-6495), a bispecific monoclonal antibody, targets IGF-1R and ErbB3 receptors and facilitates their degradation via the proteasome pathway, offering potential for cancer research [1] [2] [3].

SU-4312, also known as DMBI, is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 values are 0.8 and 19.4 μM respectively). SU4312 (SU 4312) unexpectedly protects against MPP(+) -induced neurotoxicity via selective and direct inhibition of neuronal NOS.

Robatumumab (Sch 717454), an anti-human insulin-like growth factor receptor-1 (IGF-1R) antibody, exhibits anti-tumor and anti-proliferative effects on cancer cells. It is applicable in research concerning osteosarcoma and Ewing sarcoma [1] [2].

XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).

1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib

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.

Dalotuzumab (MK-0646) is a humanized recombinant monoclonal antibody (IgG1 type) that targets IGF-1R, inhibiting tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation mediated by IGF-1 and IGF-2. It induces apoptosis and cell cycle arrest, and its antitumor activity is significantly enhanced when used alongside other anticancer agents like statins, both in vitro and in vivo [1] [2] [3].

Insulin-like Growth Factor I (24-41) TFA, a fragment comprising amino acids 24 to 41 of the full IGF-I TFA molecule, is a variant of IGF-I TFA, which itself is a 70 amino acid polypeptide hormone. This hormone serves as a trophic factor beneficial for both neurons and glial cells, playing a significant role in mediating the effects of growth hormone (GH) on systemic growth. Additionally, IGF-I TFA exhibits anabolic, antioxidant, anti-inflammatory, and cytoprotective properties. The specific fragment IGF-I (24-41) TFA is involved in regulating somatic growth as well as behavioral development [1] [2] [3].

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.

CYY292 is a chemical compound acting as an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, with respective IC50 values of 5.35, 4.6, 28, 28, and 78 nM. It exhibits selectivity over FGFR4 (IC50 > 1,000 nM) while also targeting c-Kit, VEGFR2, VEGFR1, and IGF-1R (IC50 values of 67, 33, 36, and 75 nM, respectively). Additionally, CYY292 inhibits EGFR, BTK, Cdk4/cyclin D3, and MET with IC50 values of 128, 198, 214, and 396 nM, respectively. This compound demonstrates efficacy in arresting the proliferation of various osteosarcoma cell lines—MG-63, U2OS, MNNG/HOS, and Saos-2—with IC50s ranging from 0.72 to 1.36 µM. Moreover, CYY292 at 0.3 and 0.5 µM concentrations inhibits migration and invasion in glioblastoma cells (U87MG and LN-229) and, at a dose of 30 mg/kg, decreases tumor volume and enhances survival in a U87MG orthotopic mouse xenograft model.