IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation.
性状
Solid
体外研究(In Vitro)
IXA4 (10 μM; 4 hours) selectively upregulates XBP1s mRNA, relative to genes regulated by ATF6 (e.g., BiP) or PERK (e.g., CHOP), in other cell lines including Huh7 and SHSY5Y cells. IXA4 (10μM; 18 hours) reduces Aβ levels 50% in conditioned media prepared on CHO7PA2 cells expressing the V717F APP (APPV717F) mutant. IXA4 rescues mitochondrial defects in SH-SY5Y cells expressing disease-relevant APP mutants. IXA4 (10μM; 4 hours) promotes adaptive IRE1/XBP1s signaling, but not RIDD, following 4 hrs of treatment in HEK293T cells.IXA4 also promotes selective transcriptional remodeling of ER proteostasis pathways, relative to cytosolic or mitochondrial pathways. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Grandjean JMD, et al. Pharmacologic IRE1/XBP1s activation confers targeted ER proteostasis reprogramming. Nat Chem Biol. 2020;16(10):1052-1061.
溶解度数据
In Vitro: DMSO : 100 mg/mL (229.10 mM; Need ultrasonic)配制储备液