Date published: 2026-5-15

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IGF-IIR Inhibitors

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.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

IGF-1R Inhibitor, PPP

477-47-4sc-204008A
sc-204008
sc-204008B
1 mg
10 mg
100 mg
$138.00
$203.00
$895.00
63
(1)

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

475489-16-8sc-507395
5 mg
$285.00
(0)

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

196868-63-0sc-221738
10 mg
$146.00
(1)

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)

500-38-9sc-200487
sc-200487A
sc-200487B
1 g
5 g
25 g
$109.00
$384.00
$2190.00
3
(1)

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

468740-43-4sc-507397
5 mg
$285.00
(0)

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

65678-07-1sc-205907
1 mg
$107.00
22
(1)

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

1089283-49-7sc-507398
10 mg
$321.00
(0)

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

867160-71-2sc-396762
sc-396762A
5 mg
10 mg
$146.00
$265.00
1
(0)

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.