IGF-1R

GSK1904529A selectively inhibits IGF-IR and IR with IC(50)s of 27 and 25 nmol/L, respectively.

NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM.

NVP-AEW541 is a selective IGF-1R kinase inhibitor that inhibits the autophosphorylation activity of IGF-1R (IC50 = 0.086 uM) and prevents IGF-1-mediated survival and proliferation of MCF-7 cells (IC50 = 0.16 and 1.64 uM, respectively).

OSI-906 is a potential first-in-class selective small molecule, dual kinase inhibitor of both insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR).

BMS-536924 is an effective inhibitor of IGF-IR, causing a reversion of an IGF-IR - mediated transformed phenotype.

BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively.

AG-1024 (Tyrphostin) is a specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor tyrosine kinase activity. Exhibits lower IC50 values for IGF-1 than for the insulin receptor. Also inhibits insulin-stimulated cellular proliferation.

PQ 401 is a cell-permeable phenylquinolinyl-urea compound that inhibits IGF-1R autophosphorylation.

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.

Picropodophyllin (AXL1717) is the first targeted oral small-molecule IGF-1 receptor inhibitor with no effect on the insulin receptor.

AZD-3463 is a ALK/IGF1R inhibitor.

XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.

NT157 is a selective inhibitor of IRS-1/2.

E 804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC50 of 0.65 μM for IGF1R.

SU4984 is a cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1; IC50 = 10-20 μM).

SU-4313 is a small-molecule modulator of protein tyrosine kinases (PTKs). It inhibits multiple receptor tyrosine kinases with reported IC₅₀ values of 14.5 μM (PDGFR), 18.8 μM (FLK-1/VEGFR2), 11 μM (EGFR), 16.9 μM (HER2 kinase), and 8.0 μM (IGF-1R).

Through its multi-kinase inhibitory profile, SU-4313 modulates tyrosine kinase–mediated signal transduction pathways involved in the regulation of cell proliferation and growth. It is therefore commonly used as a research tool for investigating aberrant receptor tyrosine kinase signaling and proliferation-associated pathways.

Gastric Inhibitory Peptide, porcine is a glucose-dependent insulinotropic polypeptide, is a 42 amino acid intestinal hormone with effects on fat and glucose metabolism.

[D-Ala2]-GIP (human) is a GIP receptor agonist. [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc

DA-JC4 is a dual GLP-1/GIP receptor agonist and can be used for the research of neurological disease and insulin signaling pathways.

GTx-134 is a dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR), exhibiting IC50 values of 97 nM and 187 nM, respectively. This compound effectively inhibits IGF-1R autophosphorylation and downstream Akt signaling, thereby interfering with the proliferation and survival of tumor cells. GTx-134 demonstrates broad-spectrum activity against multiple myeloma cell lines, inducing apoptosis in sensitive cells, and significantly reduces tumor growth in mouse models of myeloma. Its potential for synergistic effects with existing therapies makes GTx-134 a valuable reagent for high-risk myeloma research.

Chromeceptin (94G6) is an inhibitor of the Insulin-like Growth Factor (IGF) signaling pathway. It effectively suppresses IGF2 expression at both mRNA and protein levels in hepatocytes and hepatocellular carcinoma (HCC) cells. Additionally, Chromeceptin reduces the phosphorylation of key signaling proteins, AKT and mTOR, thereby impacting cellular growth and metabolism. This compound is valuable for research into cancer biology and therapeutic strategies targeting IGF signaling.

IGF-1R modulator 1 is a selective modulator of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting EC50 values of 0.25 μM for IGF-1R, alongside notable activity against FGFR1, TrkA, and TrkB. This compound is valuable in the study of pathological conditions associated with dysregulated signaling of neurotrophins and trophic factors, including Alzheimer's disease. Its efficacy in modulating IGF-1R offers potential insights into therapeutic approaches for neurodegenerative disorders.

AZ7550 hydrochloride is an inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with an IC50 value of 1.6 μM. This compound demonstrates significant biological activity by disrupting IGF-1R signaling, which plays a critical role in cell proliferation and survival. AZ7550 hydrochloride is primarily used in research applications focused on cancer biology, metabolic diseases, and the molecular mechanisms underlying IGF-1R-related pathways.

AZ7550 Mesylate is a potent inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting an inhibitory concentration (IC50) of 1.6 μM. It is utilized in research to study the role of IGF-1R in cellular signaling pathways, cancer proliferation, and resistance mechanisms. This compound serves as a valuable tool for understanding IGF-1R-related diseases and may aid in the development of targeted therapies.

Ginsenoside Rg5 is a potent IGF-1R agonist primarily derived from Red ginseng. It functions by competing at the IGF-1 binding site on IGF-1R, effectively obstructing IGF-1's interaction and exhibiting an IC50 of approximately 90 nM. Additionally, Ginsenoside Rg5 downregulates COX-2 mRNA expression through inhibition of NF-κB p65 DNA binding activities, making it valuable for research into inflammation and metabolic regulation.

CWI1-2 is an inhibitor of IGF2BP2 that disrupts its interaction with m6A-modified target transcripts. This compound induces apoptosis and differentiation in responsive cells, showcasing potential anti-leukemic activity. CWI1-2 is valuable for research focused on the regulation of RNA metabolism and cancer biology, particularly in leukemia studies.

AVJ16 is an inhibitor of the insulin-like growth factor 2 mRNA binding protein IGF2BP1, exhibiting a Kd of 1.4 μM. This compound disrupts the interaction between IGF2BP1 and its target mRNA, thereby modulating gene expression and translation processes. AVJ16 is valuable for research applications focused on cancer cell migration and the underlying mechanisms of IGF2BP1 in various malignancies.

I3IN-002 is a small-molecule inhibitor of the RNA-binding protein IGF2BP3, exhibiting an IC50 of approximately 2 μM in SEM cells. By disrupting the interaction with m6A-modified mRNAs, I3IN-002 destabilizes the expression of key oncogenes, such as CDK6, MYC, and BCL2, leading to inhibition of leukemic cell proliferation, induction of cell cycle arrest, and promotion of apoptosis. This compound is a valuable tool for research focused on B-cell acute lymphoblastic leukemia.

CWI1-2 hydrochloride is an inhibitor of IGF2BP2, a protein that plays a crucial role in regulating m6A-modified target transcripts. By binding to IGF2BP2, CWI1-2 hydrochloride disrupts its interaction with these transcripts, thereby inducing apoptosis and promoting differentiation in cells. This compound demonstrates significant potential for therapeutic applications in leukemia research.

IGF2BP1-IN-1 is a selective inhibitor of the insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1). It demonstrates potent inhibition of IGF2BP1 with a dissociation constant (KD) of 2.88 nM and effectively suppresses cancer cell proliferation, exhibiting IC50 values of 9 nM in A549 cells and 34 nM in HCT116 cells. Additionally, IGF2BP1-IN-1 induces apoptosis in cancer cells and has been shown to inhibit tumor growth in A549 xenograft mouse models, making it a valuable tool for cancer research and therapeutic development targeting IGF2BP1-mediated pathways.

IGF2BP3-IN-1 is an inhibitor of IGF2BP3, a RNA-binding protein essential for regulating various cellular processes. With an IC50 value greater than 50 μM, this compound is primarily utilized in cancer research to explore the role of IGF2BP3 in tumor growth and progression. Its application extends to studies investigating the influence of RNA binding proteins on gene expression and potential therapeutic pathways in oncology.

NVP-AEW541 dihydrochloride is a potent inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting an IC50 value of 0.15 μM. This compound also demonstrates inhibition of the insulin receptor (InsR) with an IC50 value of 0.14 μM. NVP-AEW541 dihydrochloride is recognized for its antitumor activity, making it a valuable tool for cancer research and therapeutic investigations targeting IGF signaling pathways.

AZD9362 is a reversible, ATP-competitive inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR). It exhibits potent biological activity with an IC50 of 14 nM for IGF-1R inhibition, making it suitable for cancer research applications. This compound has been shown to enhance the anti-tumor efficacy of AZD5363, presenting significant potential in the study of various cancers, including breast cancer.

Cis-NVP-ADW742 is a selective inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting a potent inhibitory effect with an IC50 of 0.17 μM. This compound also demonstrates a moderate inhibition of the insulin receptor (InsR) with an IC50 of 2.8 μM. Cis-NVP-ADW742 induces significant antiproliferative and pro-apoptotic effects in tumor cells, making it a valuable tool for cancer research and the study of signaling pathways involved in cell growth and survival.

KW-2450 free base is a potent inhibitor of IGF-1 receptor (IGF-1R) and acts on multiple kinases including Aurora A and B. It demonstrates significant antitumor activity against triple-negative breast cancer (TNBC) by reducing cell viability, promoting apoptosis, and inhibiting colony and mammosphere formation in TNBC cells. In vivo studies indicate that KW-2450 free base effectively suppresses the growth of TNBC xenografts, leading to apoptotic cell death or survival of polyploid cells. Additionally, it enhances the therapeutic efficacy of combination treatments with MEK inhibitors, providing a synergistic antitumor effect in various TNBC models.

KW-2450 tosylate is a selective inhibitor of the insulin-like growth factor-1 receptor (IGF-1R), as well as Aurora A and B kinases. It effectively induces apoptosis in cancer cells, demonstrating significant anticancer activity, particularly against triple-negative breast cancer. This compound is valuable for research applications involving cancer biology and therapeutic targeting of kinase signaling pathways.

IGF-1 DES is an analog of Insulin-like Growth Factor 1 (IGF-1) with a modified sequence of 83 amino acids. This peptide retains the ability to stimulate DNA synthesis, promoting follicle growth similarly to native IGF-1. It demonstrates comparable biological activity in proliferation assays, such as those conducted using NIH-3T3 cells, making it a valuable tool for research in cellular growth and development.

NBI-31772 is a non-selective inhibitor of insulin-like growth factor binding proteins (IGFBPs) with a Ki value of 47 nM. This compound exhibits neuroprotective properties and significantly reduces infarct volume during cerebral ischemia. Additionally, NBI-31772 enhances proteoglycan synthesis in osteoarticular chondrocytes and has been shown to amplify the effects of IGF3 on oocyte maturation in zebrafish. Its diverse biological activities make it a valuable tool for research in neuroprotection and chondrocyte biology.

JB-1 is a selective inhibitor of the IGF-I receptor, specifically designed to compete with IGF-I for binding at the IGF-1R site, without affecting IGF-II. This compound effectively blocks receptor autophosphorylation, leading to an increase in soluble VEGFR-1 levels. JB-1 demonstrates significant efficacy in normalizing retinal abnormalities, particularly in the context of reducing retinal neovascularization. Its application is particularly relevant for research focused on oxygen-induced retinopathy.

IGF-I (24-41) is a fragment derived from the Insulin-like Growth Factor I, encompassing amino acids 24 to 41. This peptide plays a critical role in mediating the biological effects of IGF-I, particularly in neuronal and glial cell support. IGF-I exhibits a range of biological activities, including anabolic, antioxidant, anti-inflammatory, and cytoprotective effects, making IGF-I (24-41) valuable for research in growth regulation and behavioral development studies.

AG 538 is a potent competitive inhibitor of the IGF-1 receptor kinase, with an IC50 value of 400 nM. This compound effectively blocks IGF-1 signaling pathways, which play a critical role in cell proliferation and survival. Due to its inhibitory action, AG 538 is valuable in research applications investigating cancer growth, metabolic diseases, and other conditions linked to dysregulated IGF-1 signaling.

IGF-1R inhibitor-2 is an inhibitor of the insulin-like growth factor-1 receptor (IGF-1R). This compound downregulates IGF-1R activity, which can reverse the transformed phenotype of tumor cells, thereby increasing their susceptibility to apoptosis. It is valuable for research applications focused on cancer biology and therapeutic strategies targeting IGF signaling pathways.

Mecasermin is a recombinant form of human insulin-like growth factor I (IGF-I). It primarily targets the IGF receptor and is involved in promoting cell growth and development. This compound is particularly valuable in research focused on growth disorders resulting from growth hormone insensitivity, such as those caused by defects in the growth hormone receptor or the presence of growth hormone-inhibiting antibodies.

I-OMe-Tyrphostin AG 538 is a selective inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase. This compound effectively disrupts IGF-1R-mediated signaling pathways and demonstrates preferential cytotoxicity towards nutrient-deprived PANC1 cells. Additionally, I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), exhibiting an IC50 value of 1 μM. It is valuable for research applications focused on cancer biology and metabolic stress responses.

IGF-1R/SRC-IN-1 is a selective inhibitor targeting insulin-like growth factor 1 receptor (IGF-1R) and SRC. This compound demonstrates an IC50 value of 63 μM for IGF-1R, making it a valuable tool in the study of signal transduction pathways involved in cancer and metabolic disorders. Its application extends to evaluating the role of IGF-1R and SRC in cellular proliferation, differentiation, and survival, providing insights into potential therapeutic interventions for related diseases.

AZ12253801 is an ATP-competitive inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), demonstrating approximately 10-fold selectivity over the insulin receptor. It exhibits potent inhibition of IGF-1R-mediated proliferation in 3T3 mouse fibroblasts transfected with human IGF-1R, with an IC50 value of 17 nmol/L. Additionally, AZ12253801 shows reduced activity against epidermal growth factor receptor (EGFR)-driven proliferation, with an IC50 of 440 nmol/L. Its characteristics make it a valuable tool for investigating anti-tumor mechanisms and IGF-1R signaling pathways in cancer research.

Cibrigirsen is an antisense oligonucleotide that specifically targets and reduces the expression of the insulin-like growth factor I receptor (IGF-1R). By inhibiting IGF-1R synthesis, it plays a crucial role in modulating signaling pathways associated with cell proliferation and survival. This reagent is valuable for research applications focused on cancer biology, particularly in studies investigating the role of IGF-1R in tumor growth and resistance to therapy.

IGF-1R inhibitor-3 is an allosteric inhibitor targeting insulin-like growth factor receptor 1 (IGF-1R) kinase, demonstrating an IC50 of 0.2 μM. This compound is instrumental in investigating IGF-1R signaling pathways and its role in various cancers and metabolic disorders. It has potential applications in cancer research, where modulation of the IGF-1R pathway may influence tumor growth and progression.

BMS-577098 is an orally bioavailable inhibitor of the insulin-like growth factor-1 receptor (IGF-1R), displaying an IC50 of 0.016 μM. This ATP-competitive compound demonstrates significant anti-tumor activity, making it a valuable tool in cancer research. Its inhibition of IGF-1R can aid in the exploration of therapeutic strategies targeting tumor growth and progression.