Insulin and Insulin-like Receptors

Insulin receptors (IRs) and insulin-like growth factor receptors (IGFRs) are formed from two subunits, each of which is comprised of an extracellular α-subunit and a transmembrane β-subunit with intracellular tyrosine kinase activity. IR homodimers are activated by insulin.

Products
Background
Literature
Pathways
Gene Data

Inhibitors

Cat No Product Name / Activity
4774 BMS 536924
Dual IR/IGF1R inhibitor
5111 GSK 1838705
Potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK)
5247 NVP ADW 742
ATP-competitive inhibitor of IGF1R
2956 Picropodophyllotoxin
Selective IGF1R inhibitor
2768 PQ 401
IGF1R inhibitor

Activators

Cat No Product Name / Activity
1819 Demethylasterriquinone B1
Selective insulin RTK activator
3435 Insulin (human) recombinant
expressed in yeast
Endogenous peptide agonist

Other

Cat No Product Name / Activity
5402 6bK
Insulin degrading enzyme (IDE) inhibitor
5154 HNGF6A
Humanin analog; increases insulin sensitivity
5799 Mitoglitazone
Insulin sensitizer; exhibits low binding affinity at PPARγ
5192 NBI 31772
High affinity insulin-like growth factor-I binding protein IGFBP inhibitor

Insulin receptors (IRs) and insulin-like growth factor receptors (IGFRs) are formed from two subunits, each of which is comprised of an extracellular α-subunit and a transmembrane β-subunit with intracellular tyrosine kinase activity. IR homodimers are activated by insulin and, in adults, mediate an increase in glucose uptake through upregulation of GLUT4 expression. Two isoforms of the IR exist: fetal IR-A and adult IR-B.

IGF1R homodimers are activated by IGF-I and IGF-II and mediate pre- and postnatal growth. IGF2R sequesters IGF-II and acts to regulate its levels. IR-IGF1R heterodimers exist and, similar to IGF1R homodimers, are activated by IGF-I and IGF-II. IRs and IGFRs mediate their intracellular actions through the PI3K and RAS/RAF/MAPK signaling pathways and downstream effectors include mTOR, p70 S6 kinase, ERK and JNK.

Many tumors have altered expression of IGF1R and its ligands and this constitutes an early, possible initiating, event in tumorigenesis. Decreases in IR signaling causing 'insulin resistance' is a major component in the development of type 2 diabetes and congenital mutations in the IR can cause the fatal Donohue syndrome.

Literature for Insulin and Insulin-like Receptors

Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Peptides Involved in Appetite Modulation

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Insulin and Insulin-like Receptors

Insulin

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.

Insulin and Insulin-Like Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
IR Human INSR NM_000208 P06213
Mouse Insr NM_010568 P15208
Rat Insr NM_017071 Q9WVI3
IGF1R Human IGF1R NM_000875 P08069
Mouse Igf1r NM_010513 Q60751
Rat Igf1r NM_052807 P24062
IGF2R Human IGF2R NM_000876 P11717
Mouse Igf2r NM_010515 Q07113
Rat Igf2r NM_012756 Q63002