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You are here:Home-Inhibitors & Agonists-Tyrosine Kinase-Insulin Receptor

Request The Product List ofInsulin Receptor Insulin Receptor

Insulin receptor (IR) is a transmembrane receptor that is activated by insulin, IGF-I, IGF-II and belongs to the large class of tyrosine kinase receptors. Metabolically, the insulin receptor plays a key role in the regulation of glucose homeostasis, a functional process that under degenerate conditions may result in a range of clinical manifestations including diabetes and cancer. Biochemically, the insulin receptor is encoded by a single gene INSR, from which alternate splicing during transcription results in either IR-A or IR-B isoforms. Downstream post-translational events of either isoform result in the formation of a proteolytically cleaved α and β subunit, which upon combination are ultimately capable of homo or hetero-dimerisation to produce the ≈320 kDa disulfide-linked transmembrane insulin receptor.

Cat. No. Product Name CAS No. Information
H7941

NT-157

 		1384426-12-3

A novel potential anti-cancer agent and IGF1R signaling inhibitor that targets insulin receptor substrates IRS1/2 to degradation; dose-dependently suppresses IGF1-stimulated activation of IGF1R Y980 phosphorylation (>60% at 2.5 uM) in LNCaP cells, correlated with enhanced ERK activation and IRS1/2 serine phosphorylation and degradation; suppresses CRPC progression of LNCaP xenografts, and PC3 tumor growth alone and combination with docetaxel.
H7940

MSDC-0160

 		146062-49-9

A new generation insulin sensitizer and mitochondrial target of thiazolidinediones (mTOT) modulator that has low affinity for binding and activation of PPARγ (EC50=23.7 uM) and shows insulin-sensitizing effects in mouse models of diabetes; increases AMPK activity and reduces mTOR activity, maintains β-cell phenotype in human islets.
H7939

BMS-536924

 		468740-43-4

A potent IGF-1R/InsR inhibitor with IC50 of 100 nM/73 nM; weak inhibitor of CYP3A4 (IC50=0.5 uM) and potent transactivator of PXR; increases expression and activation of various members of the HER family of receptors in ovarian cancer cell lines; causes blockade of proliferation, and results in the formation of hollow polarized lumen in MCF7 cells.

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