Chemical Name: 4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone
Biological ActivityDual inhibitor of the insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) (IC50 values are 73 and 100 nM respectively). Inhibits receptor autophosphorylation and downstream MEK1/2 and Akt signaling. Induces G1 arrest and apoptosis in ML-1 cells; also inhibits cell proliferation in multiple tumor types. Reverses EMT through the attenuation of Snail mRNA expression in MCF10A cell over expressing IGF1R.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Constitutively active type I Ins-like growth factor receptor causes transformation and xenograft growth of immortalized mammary epithelial cells and is accompanied by an epithelial-to-mesenchymal transition mediated by NF-κ
Kim et al.
Mol.Cell Biol., 2007;27:3165
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of Ins-like growth factor I receptor kinase with in vivo antitumor activity.
Wittman et al.
The mechanisms of differential sensitivity to an Ins-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors.
Huang et al.
Cancer Res., 2009;69:161
Expression of Ins receptor isoform A and Ins-like growth factor-1 receptor in human acute myelogenous leukemia: effect of the dual-receptor inhibitor BMS-536924 in vitro.
Hendrickson et al.
Cancer Res., 2009;69:7635
Citations for BMS 536924
The citations listed below are publications that use Tocris products. Selected citations for BMS 536924 include:
7 Citations: Showing 1 - 7
Activation mechanism of the Ins. receptor revealed by cryo-EM structure of the fully liganded receptor-ligand complex.
Authors: Uchikawa Et al.
The Ion Transporter NKCC1 Links Cell Volume to Cell Mass Regulation by Suppressing mTORC1.
Authors: Demian Et al.
Cell Rep 2019;27:1886
Mitotic regulators and the SHP2-MAPK pathway promote IR endocytosis and feedback regulation of Ins. signaling.
Authors: Choi Et al.
Nat Commun 2019;10:1473
Impact of ins. signaling and proteasomal activity on physiological output of a neuronal circuit in aging Drosophila melanogaster.
Authors: Augustin Et al.
Neurobiol Aging 2018;66:149
Glycolytic reliance promotes anabolism in photoreceptors.
Authors: Chinchore Et al.
Reduced ins. signaling maintains electrical transmission in a neural circuit in aging flies.
Authors: Augustin Et al.
PLoS Biol 2017;15:e2001655
Inhibition of Ins/IGF-1 receptor signaling protects from mitochondria-mediated kidney failure.
Authors: Ising Et al.
Front Behav Neurosci 2015;7:275
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