Chemical inhibitors of the insulin-like growth factor II receptor (IGF-IIR) encompass a diverse group of molecules primarily targeting signaling pathways associated with the insulin-like growth factor (IGF) system. These chemical inhibitors often do not directly interact with IGF-IIR but instead target the closely related IGF-I receptor (IGF-1R), which shares ligands and signaling pathways with IGF-IIR. IGF-IIR, which binds IGF-II, is implicated in various cellular processes, including growth regulation, and crosstalks with the IGF-1R, modulating its signaling outcomes. Inhibition of IGF-1R can indirectly decrease IGF-II-mediated signaling through IGF-IIR, either by reducing ligand availability or by interfering with the formation of receptor complexes that facilitate the signal transduction initiated by IGF-II.
The activity of these inhibitors extends beyond the simple blockade of a single signaling axis, reflecting the intricacies of cellular signaling networks. By diminishing the autophosphorylation of IGF-1R or interfering with its kinase activity, these chemicals disrupt the downstream signaling cascades that also implicate IGF-IIR. The alterations in the signaling dynamics can indirectly modulate the activity of IGF-IIR. This indirect modulation encompasses not only the reduced formation of signaling complexes involving IGF-IIR but also the attenuation of downstream signaling events that could contribute to the cellular responses mediated by IGF-IIR. Consequently, these chemical inhibitors represent a strategic approach to modulating IGF-IIR activity by targeting the broader signaling network rather than the receptor directly.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
IGF-1R Inhibitor, PPP | 477-47-4 | sc-204008A sc-204008 sc-204008B | 1 mg 10 mg 100 mg | $138.00 $203.00 $895.00 | 63 | |
PPP, an insulin-like growth factor 1 receptor (IGF-1R) inhibitor, can indirectly influence IGF-IIR by downregulating IGF-1R signaling which often crosstalks with IGF-IIR in the same pathways. Inhibition of IGF-1R leads to reduced IGF-II binding to IGF-IIR due to competition or altered receptor expression. | ||||||
NVP-AEW541 | 475489-16-8 | sc-507395 | 5 mg | $285.00 | ||
This selective IGF-1R inhibitor can attenuate the IGF-II-mediated activation of IGF-IIR through competitive inhibition. By decreasing IGF-IIR signaling, it indirectly modulates the downstream effects of IGF-IIR, such as the growth-promoting and anti-apoptotic pathways. | ||||||
PQ401 | 196868-63-0 | sc-221738 | 10 mg | $146.00 | ||
PQ401 inhibits IGF-1R autophosphorylation and its subsequent signaling. Since IGF-IIR can form a hybrid with IGF-1R, this compound may reduce the functional signaling complexes that include IGF-IIR, indirectly diminishing its activity. | ||||||
NDGA (Nordihydroguaiaretic acid) | 500-38-9 | sc-200487 sc-200487A sc-200487B | 1 g 5 g 25 g | $109.00 $384.00 $2190.00 | 3 | |
NDGA inhibits the IGF-1R tyrosine kinase, which can diminish the IGF-IIR signaling as well due to the interplay between IGF-1R and IGF-IIR. By reducing the availability of the IGF-1R for IGF-II binding, IGF-IIR signaling through the IGF-II/IGF-1R/IGF-IIR axis can be indirectly reduced. | ||||||
BMS-536924 | 468740-43-4 | sc-507397 | 5 mg | $285.00 | ||
An ATP-competitive inhibitor for IGF-1R and insulin receptor (IR), BMS-536924 may reduce IGF-II mediated signaling through IGF-IIR by limiting the availability of IGF-1R and IR, as these receptors can modulate IGF-IIR action indirectly via the formation of receptor complexes. | ||||||
AG 1024 | 65678-07-1 | sc-205907 | 1 mg | $107.00 | 22 | |
Tyrphostin AG-1024 selectively inhibits IGF-1R tyrosine kinase activity, which can reduce IGF-II action on IGF-IIR through the diminution of IGF-1R/IGF-IIR complex signaling. | ||||||
GSK1904529A | 1089283-49-7 | sc-507398 | 10 mg | $321.00 | ||
This inhibitor is specific to IGF-1R and can indirectly influence IGF-IIR by interfering with the receptor complexes that IGF-IIR may form with IGF-1R, thus impacting the signaling cascades initiated by IGF-II binding to IGF-IIR. | ||||||
Linsitinib | 867160-71-2 | sc-396762 sc-396762A | 5 mg 10 mg | $146.00 $265.00 | 1 | |
As a dual IGF-1R and IR kinase inhibitor, Linsitinib indirectly inhibits IGF-IIR by downregulating the signaling pathways shared with IGF-1R, thus potentially affecting the downstream actions of IGF-IIR. | ||||||