IRE1
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.
Targets for IRE1
Products for IRE1
- Cat.No. Product Name Information
- GC34384 3,6-DMAD hydrochloride 3,6-DMAD hydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer.
-
GC14493
4μ8C
IRE1 Rnase inhibitor, potent and non-toxic
- GC50366 AMG 18 hydrochloride AMG 18 hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
- GC17139 APY29 IRE1α inhibitor
- GC33406 B I09 B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
- GC32857 GSK2850163 GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
- GC34205 GSK2850163 hydrochloride GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
- GC63513 IRE1α kinase-IN-1 IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM.
- GC64232 IRE1α kinase-IN-2 IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines.
- GC63785 IXA4 IXA4 is a highly selective, non-toxic IRE1/XBP1s activator.
- GC64238 KIRA-7 KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity.
- GC19212 KIRA6 KIRA6 allosterically inhibits IRE1α RNase kinase activity with an IC50 of 0.6 uM.
-
GC31879
Kira8
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
- GC18303 MKC-3946 MKC-3946 is an inhibitor of inositol-requiring enzyme 1α (IRE1α).
- GC32889 MKC8866 (IRE-1α inhibitor 1) MKC8866 (IRE-1α inhibitor 1), a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29μM in human vitro. MKC8866 (IRE-1α inhibitor 1) strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52μM and unstresses RPMI 8226 cells with an IC50 of 0.14μM. MKC8866 (IRE-1α inhibitor 1) inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
- GC32910 MKC9989 MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
- GC34111 NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde) NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde) (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.
- GC12937 STF 083010 IRE1α endonuclease inhibitor
- GC17651 Sunitinib RTK inhibitor
- GC14683 Sunitinib malate A multi-kinase inhibitor
- GC48118 Sunitinib-d10 An internal standard for the quantification of sunitinib
-
GC11805
Toyocamycin
Adenosine analog,antitumor antibiotic