Merck, 412510-10MG, IRE1 Inhibitor I, STF-083010

General description
A cell-permeable salicylidene compound that is shown to directly target Ireα1 and disrupt Ire1-XBP1 (X-box binding protein) unfolded protein response (UPR) pathway in RPMI8226 multiple myeloma (MM) cells. Selectively inhibits ER stress-initiated endonuclease activity of Ire1 and blocks XPB1 mRNA splicing in MM cells at 60 µM and XBP1 activity in transgenic XBP1-luc mice (bortezomib 1mg/kg and 60 mg/kg of STF-083010, i.p.). Displays preferential cytotoxicity towards CD138+ cells over B, T and NK cells and antitumor properties.
Packaging
Packaged under inert gas
Preparation Note
Unstable in solution; reconstitute just prior to use.
Other Notes
Lerner, A.G., et al. 2012 Cell Metabolism16, 250.
Papandreou, I., et al. 2010. Blood117, )1311.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)