size : | Price | Quantity | |
---|---|---|---|
5 mg | $50.00 | ||
25 mg | $170.00 |
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 stress.1-3 It displays significant antimyeloma activity in model human MM xenografts.1 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 cancer.4 Active in vivo.
References/Citations:
1) Papandreou et al. (2011), Identification of an Ire1α 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
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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 stress.1-3 It displays significant antimyeloma activity in model human MM xenografts.1 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 cancer.4 Active in vivo.
References/Citations:
1) Papandreou et al. (2011), Identification of an Ire1α 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
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