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Home >> Signaling Pathways >> DNA Damage/DNA Repair >> IRE1

IRE1(肌醇需求酶1)

The serine/threonine-protein kinase/endoribonuclease inositol-requiring enzyme 1 (IRE1) is an enzyme that in humans is encoded by the ERN1 gene. IRE1 is an endoplasmic reticulum (ER) transmembrane sensor that activates UPR to maintain ER and cellular function. While mammalian IRE1 promotes cell survive, it can initiate apoptosis via decay of anti-apoptotic microRNAs.

IRE1 activation is initiated by homotypic interactions of the stress-sensing lumenal domain favoring transautophosphorylation of the kinase-extension nuclease (KEN) domain on the cytoplasmic side of the ER membrane.

IRE1/XBP-1 has been shown to regulate a variety of genes in various cell types in response to ER stress, mostly related to ER function and the secretory pathway, although the target genes vary depending on the cell type and nature of the stress stimuli.

Products for  IRE1

  1. Cat.No. 产品名称 Information
  2. GC64238 KIRA-7

    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。
  3. GC64232 IRE1α kinase-IN-2 IRE1α kinase-IN-2 是一种有效的 IRE1α 激酶抑制剂，EC50 为 0.82 μM。IRE1α kinase-IN-2 抑制 IRE1α 激酶自磷酸化 (IC50=3.12 μM)。IRE1α kinase-IN-2 抑制 WT 细胞系 XBP1 mRNA 剪接。
  4. GC63785 IXA4 An activator of IRE1
  5. GC63513 IRE1α kinase-IN-1 IRE1α kinase-IN-1 是一种高度选择性的 IRE1α (ERN1) 抑制剂，IC50 为 77 nM。IRE1α kinase-IN-1 对 IRE1α 的选择性比 IRE1β 亚型高 100 倍。IRE1α kinase-IN-1 抑制内质网诱导的 IRE1α 寡聚和自磷酸化，并抑制 IRE1α RNase 活性 (IC50=80 nM)。
  6. GC48118 Sunitinib-d10 An internal standard for the quantification of sunitinib
  7. GC50366 AMG 18 hydrochloride AMG 18 hydrochloride (AMG-18 Hydrochloride) 是单选择性 IRE1α；变构减弱IRE1α的抑制剂； RNase 活性，IC50 为 5.9 nM。
  8. GC34384 3,6-DMAD hydrochloride 3,6-DMADhydrochloride是未折叠蛋白质应答(IRE1α-XBP1)通路的抑制剂。
  9. GC34205 GSK2850163 hydrochloride GSK2850163hydrochloride是一个新型的肌醇需要酶-1α(IRE1α)抑制剂，它可抑制IRE1α的激酶活性和RNA酶活性，其IC50值分别为20和200nM。
  10. GC34111 NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde) 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is a bromobenzaldehyde derivative that participates in the synthesis of (±)-norannuradhapurine. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an IRE-1α inhibitor with an IC50 of 0.08 μM.
  11. GC33406 B I09 BI09是IRE-1核糖核酸酶的一个抑制剂，其IC50值为1230nM。
  12. GC32910 MKC9989

    MKC9989是一种HAA抑制剂，且能抑制IRE1α其IC50值在0.23μM至44μM的范围之间。
  13. GC32889 MKC8866 (IRE-1α inhibitor 1) MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29?μM for human IRE1α in vitro.
  14. GC32857 GSK2850163 GSK2850163是一个新型的肌醇需要酶-1α(IRE1α)抑制剂，它可抑制IRE1α的激酶活性和RNA酶活性，其IC50值分别为20和200nM。
  15. GC31879 Kira8

    Kira8 (Ire-1 inhibitor, AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  16. GC19212 KIRA6 An IRE1α RNase inhibitor
  17. GC18303 MKC-3946 An inhibitor of IRE1α
  18. GC11805 Toyocamycin A natural antibiotic and IRE1α inhibitor
  19. GC12937 STF 083010 An inhibitor of IRE1 endonuclease activity
  20. GC14493 4μ8C

    An IRE1α inhibitor
  21. GC17651 Sunitinib Sunitinib (SU 11248) 是一种多靶点受体酪氨酸激酶抑制剂，对 VEGFR2 和 PDGFRβ 的 IC50 分别为 80 nM 和 2 nM。 Sunitinib 是一种 ATP 竞争性抑制剂，通过抑制自身磷酸化和随后的 RNase 激活，有效抑制 Ire1α 的自身磷酸化。
  22. GC17139 APY29 A modulator of IRE1α function
  23. GC14683 Sunitinib malate A multi-kinase inhibitor

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