STF-083010
IRE1 ribonuclease inhibitor / A novel small molecule inhibitor of IRE1. It inhibits IRE1 endonuclease activity but not its kinase activity after endoplasmic reticulum stress1-3. It displays significant antimyeloma activity in model human MM xenografts1. Induces apoptosis in pancreatic cancer cells and displays growth inhibition in a clonogenic growth assay in soft agar as well as in a xenograft in vivo model of pancreatic cancer4. Active in vivo.
Biochemicals & reagents
307543-71-1
1) Papandreou et al. (2011), Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma; Blood, 117 1311 2) Wang et al. (2012), Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors; Nature Chem. Biol., 8 982 3) Tam et al. (2014), Ire1 has distinct catalytic mechanisms for XBP/HAC1 splicing and RIDD; Cell Rep., 9 850 4) Chien et al. (2014), Selective inhibition of unfolded protein response induces apoptosis in pancreatic cancer cells; Oncotarget, 5 4881
RT
TARGET: RNA; UPR (Unfolded Protein Response) -- PATHWAY: Apoptosis inducer; Transcription -- RESEARCH AREA: Cellular stress; Cell death -- DISEASE AREA: Cancer