Insulin II Inhibitors
Chemical inhibitors of Insulin II play a role in modulating the function of this protein by interfering with its signaling pathways. BMS-754807 and linsitinib, both inhibitors of the insulin-like growth factor 1 receptor (IGF-1R), act to impair the cross-talk between IGF-1R and Insulin II receptor signaling pathways. By doing so, these inhibitors reduce the autophosphorylation of IGF-1R, which is necessary for the downstream activation of Insulin II functions. Picropodophyllin also targets IGF-1R, but it specifically inhibits its autophosphorylation without affecting the insulin receptor, thereby indirectly decreasing Insulin II signaling. Nordihydroguaiaretic acid (NDGA) inhibits protein tyrosine kinases that are essential for the phosphorylation of the Insulin II receptor, consequently interrupting the Insulin II signaling cascade.
Tyrphostin AG 538 and S961 target the insulin receptor directly, which shares structural and functional characteristics with the Insulin II receptor. Tyrphostin AG 538 inhibits the tyrosine kinase activity of the insulin receptor, which is also involved in Insulin II signal transduction. S961 acts as a peptide antagonist to the insulin receptor, which informs the development of small-molecule inhibitors that could target the Insulin II receptor in a similar fashion. Furthermore, PQ401 and OSI-906 inhibit the autophosphorylation of IGF-1R and, in the case of OSI-906, the insulin receptor as well, leading to a dual inhibition effect on the signaling pathways that Insulin II relies on. GNF-2, an allosteric inhibitor of Bcr-Abl, can decrease Insulin II signaling by interfering with insulin receptor substrate proteins that are necessary for Insulin II signal transduction. GNF-5837, although it is a selective inhibitor for the Trk family of receptor tyrosine kinases, can affect Insulin II by diminishing insulin receptor substrate phosphorylation due to signaling cross-talk. Lastly, PF-06424439, an inhibitor of diacylglycerol O-acyltransferase 1 (DGAT1), can indirectly affect Insulin II signaling by altering the lipid metabolism and the cellular lipid environment, which is important for the localization and function of the Insulin II receptor.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
BMS-754807 | 1001350-96-4 | sc-507396 | 5 mg | $304.00 | ||
BMS-754807 is a potent and reversible inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), which is known to cross-talk with the insulin signaling pathway. By inhibiting IGF-1R, BMS-754807 can reduce the signaling cascade that may lead to decreased insulin receptor substrate activity, thereby inhibiting Insulin II signaling. | ||||||
Linsitinib | 867160-71-2 | sc-396762 sc-396762A | 5 mg 10 mg | $143.00 $260.00 | 1 | |
Linsitinib is another inhibitor of IGF-1R, which shares significant structural and functional homology with the Insulin II receptor. By inhibiting IGF-1R, linsitinib impairs the cross-talk between IGF-1R and Insulin II receptor signaling pathways, leading to reduced insulin receptor activation and subsequent inhibition of Insulin II functions. | ||||||
IGF-1R Inhibitor, PPP | 477-47-4 | sc-204008A sc-204008 sc-204008B | 1 mg 10 mg 100 mg | $112.00 $199.00 $877.00 | 63 | |
Picropodophyllin is a selective inhibitor of IGF-1R, impairing the IGF-1R autophosphorylation without affecting the insulin receptor directly. This inhibition can diminish the downstream signaling of Insulin II by limiting the cross-talk and the potential phosphorylation of shared substrates, thus indirectly inhibiting Insulin II activity. | ||||||
NDGA (Nordihydroguaiaretic acid) | 500-38-9 | sc-200487 sc-200487A sc-200487B | 1 g 5 g 25 g | $107.00 $376.00 $2147.00 | 3 | |
Nordihydroguaiaretic acid (NDGA) inhibits protein tyrosine kinases, which are crucial for insulin signal transduction. By inhibiting these kinases, NDGA can interfere with the phosphorylation of the Insulin II receptor and its substrates, leading to inhibition of Insulin II signaling pathways. | ||||||
AG-490 | 133550-30-8 | sc-202046C sc-202046A sc-202046B sc-202046 | 5 mg 50 mg 25 mg 10 mg | $82.00 $323.00 $219.00 $85.00 | 35 | |
Tyrphostin AG 538 is known to inhibit the insulin receptor tyrosine kinase. While its primary target is the insulin receptor, due to the structural similarity to the Insulin II receptor, it can inhibit the tyrosine kinase activity associated with Insulin II, thus blocking its signal transduction. | ||||||
PQ401 | 196868-63-0 | sc-221738 | 10 mg | $146.00 | ||
PQ401 inhibits the autophosphorylation of the IGF-1R. This inhibition decreases the downstream signaling that could possibly contribute to Insulin II signal transduction by reducing cross-activation of the Insulin II receptor, thus indirectly inhibiting Insulin II activity. | ||||||
GNF 5837 | 1033769-28-6 | sc-490003 | 5 mg | $79.00 | 1 | |
GNF-5837 is a potent and selective inhibitor of the Trk family of receptor tyrosine kinases. The Trk receptors can engage in signaling cross-talk with the insulin receptor pathways. Inhibition of Trk receptors could lead to decreased insulin receptor substrate phosphorylation, indirectly inhibiting Insulin II. | ||||||