Search Result
Results for "
IRES
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-124811
-
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c-Myc
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Cancer
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IRES-C11 is a spectfic c-MYC internal ribosome entry site (IRES) translation inhibitor. IRES-C11 blocks the interaction of a requisite c-MYC IRES trans-acting factor, heterogeneous nuclear ribonucleoprotein A1, with its IRES. IRES-C11 does not inhibits BAG-1, XIAP and p53 IRESes .
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- HY-135902A
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NSC 377363 hydrochloride
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DNA/RNA Synthesis
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Neurological Disease
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Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease .
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- HY-136735
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IRE1
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Neurological Disease
Cancer
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IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) .
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- HY-135902
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NSC 377363
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DNA/RNA Synthesis
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Neurological Disease
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Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease .
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- HY-153474
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IRE1
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Others
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IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent IRE-1α inhibitor. IRE1α kinase-IN-8 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) .
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- HY-158393
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IRE1
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Cancer
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IRE1a-IN-2 (Compound 30) is an IRE1α inhibitor, with an IC50 of over than 200 nM for XBP1 mRNA. IRE1a-IN-2 can be used for the research of cancer .
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- HY-158386
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IRE1
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Cancer
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IRE1a-IN-1 (Compound 10) is an IRE1α inhibitor, with an IC50 of less than 100 nM for XBP1 mRNA. IRE1a-IN-1 can be used for the research of cancer .
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- HY-153475
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IRE1
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Cancer
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IRE1α kinase-IN-9 (compound 2) is a potent IRE-1α inhibitor,exhibits an average IC50 value of <0.1 μM. IRE1α kinase-IN-9 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) .
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- HY-145419
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IRE1
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Others
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IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α .
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- HY-145420
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IRE1
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Others
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IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α .
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- HY-145418
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IRE1
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Others
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IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α .
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- HY-153713
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PROTACs
c-Myc
Apoptosis
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Cancer
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MYC-RIBOTAC is a nucleic acid-targeting degrader (ribonuclease-targeting chimera, RIBOTAC) that targets the MYC internal ribosome entry site (IRES). MYC-RIBOTAC contains a MYC mRNA binding component and a small molecule that recruits and locally activates RNAse L1. MYC-RIBOTAC reduces MYC mRNA and protein expression levels, induces cell apoptosis, and can be used for antitumor research . MYC-RIBOTAC consists of pre-miR-155 binder Anticancer agent 167 (HY-156839), RNA binder NCI-B16 (HY-156215), and Linker Amino-PEG4-alcohol (HY-W008005).
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- HY-139212
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IRE1
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Others
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IXA6 is a novel IRE1/XBP1s activator, and can induce IRE1 RNase activity .
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- HY-107400
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B I09
1 Publications Verification
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IRE1
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Cancer
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B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
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- HY-18509
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IRE1
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Cancer
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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 .
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- HY-172216
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Enterovirus
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Infection
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EV-A71-IN-3 (Compound IRE-03-3) is the inhibitor for Enterovirus A71 EV-A71 that targets internal ribosomal entry site (IRES) of EV-A71, inhibits IRES-mediated translation, and inhibits the viral proliferation with an EC50 of 11.96 μM .
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- HY-19707
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IRE1 Inhibitor III
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IRE1
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Metabolic Disease
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4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
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- HY-129348
-
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IRE1
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Cancer
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IRE1α kinase-IN-10 (GP29) is an IRE1α kinase inhibitor. IRE1α kinase-IN-10 can be used for the research of endoplasmic reticulum stress-related diseases .
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- HY-18510
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IRE1
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Others
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IRE1α kinase-IN-7 (compound 4) is an IRE1α kinase inhibitor. IRE1α kinase-IN-7 can be used for research of endoplasmic reticulum stress-related diseases .
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- HY-139214
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IXA4
2 Publications Verification
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IRE1
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Neurological Disease
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IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation .
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- HY-142659
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IRE1
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Cancer
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IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.
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- HY-U00460
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IRE1
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Cancer
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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 .
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- HY-U00460B
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IRE1
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Cancer
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3,6-DMAD dihydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer .
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- HY-145425
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IRE1
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Cancer
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PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing .
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- HY-17537
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IRE1
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Cancer
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APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
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- HY-107371
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NSC95682
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IRE1
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Cancer
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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.
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- HY-162075
-
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Biochemical Assay Reagents
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Others
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RF16 is a fluorescent macromolecular material. RF16 precisely retains in cells to track IRE1-Halo protein with the HaloTag ligand .
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- HY-114368A
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AMG-18 Hydrochloride
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IRE1
|
Inflammation/Immunology
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Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
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- HY-114368
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AMG-18
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IRE1
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Inflammation/Immunology
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Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
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- HY-169763
-
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IRE1
Apoptosis
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Cancer
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D-F07 is a prodrug with an aldehyde shielding group and an IRE-1 inhibitor that induces Apoptosis. D-F07 has antitumor activity .
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- HY-15845
-
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IRE1
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Cancer
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STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
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- HY-U00459
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IRE1
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Cancer
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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.
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- HY-U00459B
-
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IRE1
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Cancer
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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.
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- HY-103248
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Vengicide
|
IRE1
Fungal
Antibiotic
Apoptosis
CDK
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Infection
Cancer
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Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
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- HY-19710
-
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IRE1
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Cancer
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MKC3946 is a potent IRE1α inhibitor, used for cancer research.
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- HY-114611
-
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IRE1
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Metabolic Disease
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BDM44768 is an inhibitior of IDE. BDM44768 exacerbates ER stress-induced IRE1 activation and promotes lipid accumulation in hepatocytes. BDM44768 potentiates activation of the IRE1 pathway in the liver and exacerbates liver lipid accumulation in an acute mice model of ER stress .
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- HY-145422
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IRE1
Apoptosis
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Others
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KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis .
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- HY-161672
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Liposome
IRE1
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Cancer
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G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown .
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- HY-101931
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VEGFR
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Cancer
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hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression .
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- HY-12399
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MKC9989
1 Publications Verification
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IRE1
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Cancer
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MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
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- HY-169939
-
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IRE1
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Cancer
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1ACTA is an IRE1α S-Nitrosylation inhibtor, maintaining the endoplasmic reticulum stress response under nitrosative stress .
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- HY-U00459A
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IRE1
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Others
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GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
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- HY-19708
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- HY-124646
-
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IRE1
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Inflammation/Immunology
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KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect .
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- HY-153837A
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HCV
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Infection
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ISIS 14803 sodium is a 20-unit antisense phosphorothioate oligodeoxynucleotide that binds to hepatitis C virus (HCV) RNA at the translation initiation region of the internal ribosome entry site (IRES) and inhibits protein expression in cell culture.
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- HY-153837
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HCV
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Infection
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ISIS 14803 is a 20-unit antisense phosphorothioate oligodeoxynucleotide that binds to hepatitis C virus (HCV) RNA at the translation initiation region of the internal ribosome entry site (IRES) and inhibits protein expression in cell culture.
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- HY-104040
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Orin1001
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IRE1
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Cancer
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MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM . MKC8866 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 .
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- HY-153773
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Z4P
3 Publications Verification
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IRE1
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Cancer
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Z4P is a BBB-penatrable IRE1 inhibitor with an IC50 of 1.13 μM. Z4P in combination with Temozolomide (HY-17364) inhibits the growth and recurrence of glioblastoma and has anti-tumor activity .
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- HY-10255A
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Sunitinib
Maximum Cited Publications
64 Publications Verification
SU 11248
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VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
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Cancer
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Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
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- HY-10255
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SU 11248 Malate
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PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
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Cancer
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Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
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- HY-10255AS
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SU 11248-d10
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VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
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Cancer
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Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
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- HY-10255AS1
-
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Isotope-Labeled Compounds
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
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Cancer
|
Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
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- HY-10255AR
-
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VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
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Cancer
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Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
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- HY-10255R
-
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PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
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Cancer
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Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
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- HY-145932
-
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Enterovirus
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Infection
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DMA-135 hydrochloride inhibits enterovirus 71 (EV71) IRES-dependent translation and replication. DMA-135 hydrochloride binds to enterovirus 71 (EV71) SLII domain with moderately high affinity (KD= 520 nM). DMA-135 hydrochloride has no significant toxicity in cell-based studies . DMA-135 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-170849
-
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Nuclear Hormone Receptor 4A/NR4A
Apoptosis
PERK
IRE1
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Cancer
|
Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. Nur77 modulator 4 significantly induces Nur77 expression and apoptosis, showing excellent growth inhibition in HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, thereby inducing cell apoptosis. Nur77 modulator 4 can be used in cancer research applications .
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HY-L054
-
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268 compounds
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Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer.
MCE Endoplasmic Reticulum Stress Compound Library contains 268 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.
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Cat. No. |
Product Name |
Type |
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- HY-162075
-
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Fluorescent Dyes/Probes
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RF16 is a fluorescent macromolecular material. RF16 precisely retains in cells to track IRE1-Halo protein with the HaloTag ligand .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10255AS
-
|
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
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-
-
- HY-10255AS1
-
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Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
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Cat. No. |
Product Name |
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Classification |
-
- HY-153837A
-
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Antisense Oligonucleotides
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ISIS 14803 sodium is a 20-unit antisense phosphorothioate oligodeoxynucleotide that binds to hepatitis C virus (HCV) RNA at the translation initiation region of the internal ribosome entry site (IRES) and inhibits protein expression in cell culture.
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- HY-153837
-
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Antisense Oligonucleotides
|
ISIS 14803 is a 20-unit antisense phosphorothioate oligodeoxynucleotide that binds to hepatitis C virus (HCV) RNA at the translation initiation region of the internal ribosome entry site (IRES) and inhibits protein expression in cell culture.
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