STF-083010 (307543-71-1) is 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. STF-083010 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.
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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