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 (10):

目录号 产品名 作用方式 纯度
  • HY-10255A
    Sunitinib Inhibitor ≥98.0%
    Sunitinib (SU 11248) 是一种多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR2PDGFRβIC50 分别为 80 nM 和 2 nM。Sunitinib 是ATP 竞争性抑制剂,可通过抑制自身磷酸化和随后的 RNase 激活来有效抑制 Ire1α 的磷酸化。
  • HY-19707
    4μ8C Inhibitor 99.72%
    4μ8C (IRE1 Inhibitor III)是IRE1α的小分子抑制剂。
  • 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-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 99.55%
    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。
  • HY-124646
    KIRA-7 Inhibitor
    KIRA-7 是一种咪唑并吡嗪化合物,可与 IRE1α 激酶结合 (IC50 为 110 nM) 以变构方式抑制其 RNase 活性。KIRA-7 具有抗纤维化作用。
  • HY-114368A
    Kira8 Hydrochloride Inhibitor
    Kira8 Hydrochloride (AMG-18 Hydrochloride) 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-10255AS
    Sunitinib D10 Inhibitor
    Sunitinib D10 (SU 11248 D10) 是 Sunitinib 的氘代物。Sunitinib 是一种多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR2PDGFRβIC50 分别为 80 nM 和 2 nM。Sunitinib 是ATP 竞争性抑制剂,可通过抑制自身磷酸化和随后的 RNase 激活来有效抑制 Ire1α 的磷酸化。
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