Background
In cells undergoing endoplasmic reticulum (ER) stress, the cell-permeable compound STF-083010 specifically inhibits inositol-requiring enzyme-1 (IRE1) RNase activity and blocks prolonged unfolded protein response (UPR) initiation. IRE1α-mediated splicing of X-box binding protein 1 (XBP1) mRNA induces expression of many UPR responsive genes. In a rat model of acute renal failure, STF-083010 treatment suppressed oxidative stress, inflammation, and apoptosis. These cellular changes coincided with reduced impairment of kidney structure and function. By inhibiting IRE1, STF-083010 prevented prolonged UPR and downregulated expression of GRP78, p-IRE1, XBP1s, CHOP, and caspase-3 (1). In a model of multiple myeloma xenografts under ER stress, STF-083010 inhibited IRE1 endonuclease activity and showed significant anti-myeloma activity (2). STF-083010 treatment in pancreatic cancer cell lines caused growth arrest at either the G1 or G2/M phases and induced apoptosis (3). Similar therapeutic results were seen as STF-083010 prevented thioacetamide-induced acute liver injury by reducing reactive oxygen species production and decreasing hepatic inflammation (4).
Molecular Formula
C15H11NO3S2
Molecular Weight
317.4 g/mol
Purity
>98%
CAS
307543-71-1
Solubility
Soluble in DMSO at 30 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
限制使用
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