Chemical Name: 4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone
Biological ActivityBMS 536924 is a dual 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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
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
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
No product specific FAQs exist for this product, however you mayView all Small Molecule FAQs
VersaClone cDNA Plasmids
Reviews for BMS 536924
There are currently no reviews for this product. Be the first to review BMS 536924 and earn rewards!
Have you used BMS 536924?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image