Description
Product Usage Information
STF-083010 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 1.05 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles .
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).
Alternate Names
N-[(2-Hydroxy-1-naphthalenyl)methylene]-2-thiophenesulfonamide
