1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Insulin Receptor

Insulin Receptor

Insulin receptor (IR), a phylogenetically ancient tyrosine kinase receptor, is a large cell surface glycoprotein that concentrates insulin at the site of action and also initiates responses to insulin. The receptor is a disulfide-linked oligomer comprised of two alpha and two beta subunits. The insulin receptor exists in two isoforms, IR-A and IR-B, expressed in different relative abundance in the various organs and tissues. The two IR isoforms have similar binding affinity for insulin but different affinity for insulin-like growth factor (IGF)-2 and proinsulin, which are bound by IR-A but not IR-B.

The insulin receptor has a crucial role in controlling glucose homeostasis, regulating lipid, protein and carbohydrate metabolism, and modulating brain neurotransmitter levels. Insulin receptor dysfunction has been associated with many diseases, including diabetes, cancer and Alzheimer's disease.

Insulin Receptor Related Products (46):

Cat. No. Product Name Effect Purity
  • HY-P0035
    Insulin (human)
    Insulin (human) is a polypeptide hormone that regulates the level of glucose.
  • HY-P1156
    Insulin(cattle)
    ≥98.0%
    Insulin cattle (Insulin from bovine pancreas) is a two-chain polypeptide hormone produced in vivo in the pancreatic β cells. Insulin cattle has often been used as growth supplement in culturing cells.
  • HY-10191
    Linsitinib
    Inhibitor 99.83%
    Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively.
  • HY-15656
    Ceritinib
    Inhibitor 99.97%
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
  • HY-10200
    BMS-754807
    Inhibitor 99.76%
    BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively.
  • HY-145935
    NT219
    Inhibitor
    NT219 is a potent and dual inhibitor of insulin receptor substrates 1/2 (IRS1/2) and STAT3. IRS1/2 and STAT3 are major signaling junctions regulated by various oncogenes. NT219 affects IRS1/2 degradation and inhibits STAT3 phosphorylation. NT219 has the potential for the research of cancer diseases.
  • HY-144873
    AVJ16
    99.67%
    AVJ16 is a member of the insulin-like growth factor 2 mRNA-binding protein family. AVJ16 regulates protein translation by binding to the mRNAs of certain genes.
  • HY-W040127
    Peonidin 3-O-glucoside chloride
    Peonidin 3-O-glucoside chloride, an anthocyanin, act as an insulin secretagogue. Peonidin 3-O-glucoside chloride can increase glucose uptake in HepG2 cells. Peonidin 3-O-glucoside chloride has the potential for type-2 diabetes comorbidities research.
  • HY-10262
    BMS-536924
    Inhibitor 99.83%
    BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.
  • HY-10524
    GSK1904529A
    Inhibitor 99.66%
    GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
  • HY-50866
    NVP-AEW541
    Inhibitor ≥99.0%
    NVP-AEW541 (AEW541) is a potent inhibitor of IGF-1R with IC50 of 0.15 μM, also inhibits InsR, with IC50 of 0.14 μM.
  • HY-P2093B
    S961 acetate
    Antagonist 99.52%
    S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
  • HY-13020
    GSK1838705A
    Inhibitor 98.95%
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
  • HY-100550
    MSDC 0160
    Modulator 99.40%
    MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulating insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease.
  • HY-15656A
    Ceritinib dihydrochloride
    Inhibitor 99.83%
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-13203
    NVP-TAE 226
    Inhibitor 99.92%
    NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
  • HY-10253
    AG1024
    Inhibitor 99.82%
    AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
  • HY-10252
    NVP-ADW742
    Inhibitor 99.30%
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
  • HY-P0276A
    GIP, human TFA
    Agonist
    GIP, human TFA, a peptide hormone consisting of 42 amino acids, is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP, human TFA acts as an incretin hormone released from intestinal K cells in response to nutrient ingestion.
  • HY-N0755
    Rhoifolin
    Activator 99.24%
    Rhoifolin is a flavone glycoside can be isolated from Citrus grandis (L.) Osbeck leaves. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.