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Cell Cycle/Checkpoint Cell Cycle/CheckpointIRE1
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.
- D-F07T843112361297-58-5In houseD-F07 is a novel fluorescent IRE-1 RNase inhibitor and a tricyclic chromone with potential anticancer activity.
- $195
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- APY29T36541216665-49-4APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
- $36
SizeQTY
Cited - 4μ8CT636314003-96-44μ8C (IRE1 Inhibitor III)(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
- $43
SizeQTY Cited - ToyocamycinT17143606-58-6Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.
- $39
SizeQTY - IXA4T93491185329-96-7IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreatic function.
- $34
SizeQTY - SunitinibT0374L557795-19-4Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.
- $53
SizeQTY Cited - MKC3946TQ01011093119-54-0MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
- $61
SizeQTY - B I09T148471607803-67-7In houseB I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells.
- $44
SizeQTY - IXA6T625681021106-40-0IXA6, a novel IRE1 XBP1s agonist with potential vasoprotective activity, activates IRE1-XBP1s signaling and XBP1s transcriptional response, making it useful for studying neurodegenerative diseases such as Parkinson's disease and Alzheimer's disease.
- $299
SizeQTY - IRE1α kinase-IN-1T95642328097-41-0IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM, displaying 100-fold selectivity over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, as well as IRE1α RNase activity (IC50=80 nM).
- $118
SizeQTY - Kira8T11762L1630086-20-2Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
- $89
SizeQTY - MKC8866T155941338934-59-0MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.
- $48
SizeQTY - Sunitinib MalateT0374341031-54-7Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80 2 nM), and c-kit.
- $37
SizeQTY - GSK2850163T114882121989-91-9In houseGSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).
- $64
SizeQTY - KIRA6TQ00761589527-65-0KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.
- $39
SizeQTY Cited - STF-083010T6681307543-71-1STF-083010 is a selective inhibitor of the IRE1α endonuclease.
- $47
SizeQTY Cited - 6-Bromo-2-hydroxy-3-methoxybenzaldehydeT748320035-41-06-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC-95682) is an inhibitor of IRE-1α with an IC50 value of 0.08 μM.
- $34
SizeQTY - GSK2850163 (S enantiomer)T98482309519-81-9In houseGSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).
- $117
SizeQTY - MKC9989T120711338934-20-5MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
- $47
SizeQTY - IRE1α kinase-IN-9T790631338933-30-4IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α with an average IC50 value of less than 0.1 μM, and it is suitable for research into diseases related to the unfolded protein response or regulated IRE1-dependent decay (RIDD) [1].
- $1,520
SizeQTY - IRE1α kinase-IN-8T790621338933-29-1IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent inhibitor of IRE-1α used in research on diseases related to the unfolded protein response and regulated IRE1-dependent decay (RIDD) [1].
- $1,520
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