Linsitinib is highly potent, orally efficacious and highly selective, dual ATP-competitive inhibitor of IGF-1R (IC50= 35 nM) and insulin receptor (IC50=75 nM).

Gastric Inhibitory Peptide (GIP), human is thought to act as an inhibitor of gastric functions. It also affects lipid metabolism and displays mitogenic and antiapoptotic effects in pancreatic β-cells.

Tolazamide is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity.

MSDC-0160 is a prototype mTOR-modulating insulin sensitizer being studied to treat diabetes and Alzheimer's disease.

Ceritinib is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.

Rhoifolin, a natural product isolated and purified from the leaves of Turpinia arguya Seem, hows monolithic proliferation inhibitory activities against Hela, A549 and MCF-7 cell lines, and may be beneficial for diabetic complications through their enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and GLUT4. It was found to efficiently block the enzymatic activity of SARS-CoV 3CLpro.

Kaempferitrin can activate insulin signaling pathway, phosphorylate Akt kinase and exert the transloocation of GLUT4, thus has antitumor, antidepressant and antidiabetic effects. Kaempferitrin is a natural product isolated and purified from the root of Kaempferia galangal L..

BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM.

NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 86 nM, 27-fold greater selectivity for IGF-1R than InsR.

Cinnamic acid can stimulate insulin secretion and improve glucose tolerance.

BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc.