1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. IRE1

IRE1 (肌醇需求酶1)

Inositol-requiring enzyme 1 (IRE1) is a bifunctional serine/threonine kinase and endoribonuclease that is a major mediator of the unfolded protein response (UPR) during endoplasmic reticulum (ER) stress. It represents a potential therapeutic target for a number of diseases associated with endoplasmic reticulum stress.

IRE1 is the only identified ER stress sensor in yeast and essential for UPR in animals and plants. As an ER transmembrane protein, IRE1 monitors ER homeostasis through an ER luminal stress-sensing domain and triggers UPR through a cytoplasmic kinase domain and an RNase domain. Upon ER stress, IRE1 RNase is activated through conformational change, autophosphorylation, and higher order oligomerization. Mammalian IRE1 initiates diverse downstream signaling of the UPR either through unconventional splicing of the transcription factor Xbp-1 or and through posttranscriptional modifications via Regulated IRE1-Dependent Decay (RIDD) of multiple substrates.

IRE1 相关产品 (6):

Cat. No. Product Name Effect Purity
  • HY-15845
    STF-083010 Inhibitor ≥98.0%
    STF-083010 是一种 IRE1α 特异性抑制剂。在内质网应激后,STF-083010 抑制 Ire1 内切核酸酶活性,而不影响其激酶活性。
  • HY-19707
    4μ8C Inhibitor 99.72%
    4μ8C (IRE1 Inhibitor III)是IRE1α的小分子抑制剂。
  • HY-114368
    Kira8 Inhibitor 99.74%
    Kira8 (AMG-18) 是一种单选择性 IRE1α 抑制剂,可以变构减弱 IRE1α RNase 活性,IC50 为 5.9 nM。
  • HY-103248
    Toyocamycin Inhibitor ≥99.0%
    Toyocamycin (Vengicide) 是放线菌类产生的腺苷类似物,为 X 盒结合蛋白 1 (XBP1) 抑制剂,抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 的断裂,IC50 值为 80 nM。Toyocamycin (Vengicide) 诱导凋亡,对 IRE1α 的自身磷酸化没有作用。
  • HY-107371
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde Inhibitor 99.87%
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) 是一个 IRE-1α 抑制剂,其 IC50 值为 0.08 μM,来自专利 WO 2008154484 A1, 实例 IRE-lα 抑制剂化合物 3-5。
  • HY-U00460
    3,6-DMAD hydrochloride Inhibitor ≥99.0%
    3,6-DMAD hydrochloride是未折叠蛋白质应答 (IRE1α-XBP1) 通路的抑制剂。
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