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IRES

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44

Inhibitors & Agonists

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Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-124811

    c-Myc Cancer
    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 .
    <em>IRES</em>-C11
  • HY-153713

    c-Myc Apoptosis Cancer
    MYC-RIBOTAC is a ribonuclease-targeting chimera (RIBOTAC) to MYC internal ribosome entry site (IRES).MYC-RIBOTAC contains a MYC mRNA-binder and a small molecule that recruits and locally activates RNase L1 and decreases the mRNA and protein expression levels of MYC, induces apoptosis. MYC-RIBOTAC can be used for anticancer research .
    MYC-RIBOTAC
  • HY-135902A

    NSC 377363 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    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 .
    Synucleozid hydrochloride
  • HY-135902

    NSC 377363

    DNA/RNA Synthesis Neurological Disease
    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 .
    Synucleozid
  • HY-153474

    IRE1 Others
    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) .
    <em>IRE</em>1α kinase-IN-8
  • HY-136735

    IRE1 Neurological Disease Cancer
    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) .
    <em>IRE</em>1α kinase-IN-1
  • HY-153475

    IRE1 Cancer
    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) .
    <em>IRE</em>1α kinase-IN-9
  • HY-145418

    IRE1 Others
    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 .
    <em>IRE</em>1α kinase-IN-3
  • HY-145419

    IRE1 Others
    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 .
    <em>IRE</em>1α kinase-IN-4
  • HY-145420

    IRE1 Others
    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 .
    <em>IRE</em>1α kinase-IN-5
  • HY-139212

    IRE1 Others
    IXA6 is a novel IRE1/XBP1s activator, and can induce IRE1 RNase activity .
    IXA6
  • HY-107400
    B I09
    1 Publications Verification

    IRE1 Cancer
    B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
    B I09
  • HY-18509

    IRE1 Cancer
    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 .
    <em>IRE</em>1α kinase-IN-2
  • HY-19707
    4μ8C
    30+ Cited Publications

    IRE1 Inhibitor III

    IRE1 Metabolic Disease
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
    4μ8C
  • HY-18510

    IRE1 Others
    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 .
    <em>IRE</em>1α kinase-IN-7
  • HY-139214
    IXA4
    2 Publications Verification

    IRE1 Neurological Disease
    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 .
    IXA4
  • HY-142659

    IRE1 Cancer
    IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.
    <em>IRE</em>1α kinase-IN-6
  • HY-U00460

    IRE1 Cancer
    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 .
    3,6-DMAD hydrochloride
  • HY-U00460B

    IRE1 Cancer
    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 .
    3,6-DMAD dihydrochloride
  • HY-145425

    IRE1 Cancer
    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 .
    PAIR2
  • HY-17537
    APY29
    5+ Cited Publications

    IRE1 Cancer
    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 .
    APY29
  • HY-107371

    NSC95682

    IRE1 Cancer
    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.
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde
  • HY-114368A

    AMG-18 Hydrochloride

    IRE1 Inflammation/Immunology
    Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
    Kira8 Hydrochloride
  • HY-114368
    Kira8
    5+ Cited Publications

    AMG-18

    IRE1 Inflammation/Immunology
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
    Kira8
  • HY-15845
    STF-083010
    30+ Cited Publications

    IRE1 Cancer
    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
    STF-083010
  • HY-U00459
    GSK2850163
    3 Publications Verification

    IRE1 Cancer
    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.
    GSK2850163
  • HY-U00459B

    IRE1 Cancer
    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.
    GSK2850163 hydrochloride
  • HY-103248
    Toyocamycin
    4 Publications Verification

    Vengicide

    IRE1 Fungal Antibiotic Apoptosis CDK Infection Cancer
    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 .
    Toyocamycin
  • HY-19710
    MKC3946
    5 Publications Verification

    IRE1 Cancer
    MKC3946 is a potent IRE1α inhibitor, used for cancer research.
    MKC3946
  • HY-145422

    IRE1 Apoptosis Others
    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 .
    KIRA9
  • HY-101931

    VEGFR Cancer
    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 .
    hVEGF-IN-1
  • HY-12399

    IRE1 Cancer
    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
    MKC9989
  • HY-U00459A

    IRE1 Others
    GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
    GSK2850163 (S enantiomer)
  • HY-19708
    KIRA6
    10+ Cited Publications

    IRE1 Metabolic Disease Inflammation/Immunology Cancer
    KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM . KIRA6 can trigger an apoptotic response .
    KIRA6
  • HY-124646

    IRE1 Inflammation/Immunology
    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 .
    KIRA-7
  • HY-153837

    HCV Infection
    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.
    ISIS 14803
  • HY-153837A

    HCV Infection
    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.
    ISIS 14803 sodium
  • HY-104040
    MKC8866
    5+ Cited Publications

    Orin1001

    IRE1 Cancer
    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 .
    MKC8866
  • HY-153773

    IRE1 Cancer
    Z4P is a BBB-permeable IRE1 inhibitor (IC50: 1.11 μM). Z4P inhibits Glioblastoma cell growth. Z4P prevents glioblastoma relapse when administered together with Temozolomide (HY-17364) .
    Z4P
  • HY-10255A
    Sunitinib
    Maximum Cited Publications
    46 Publications Verification

    SU 11248

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    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 .
    Sunitinib
  • HY-10255
    Sunitinib Malate
    Maximum Cited Publications
    46 Publications Verification

    SU 11248 Malate

    PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    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 .
    Sunitinib Malate
  • HY-10255AS

    SU 11248-d10

    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].
    Sunitinib-d10
  • HY-10255AS1

    Isotope-Labeled Compounds VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis 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].
    Sunitinib-d4
  • HY-145932

    Enterovirus Infection
    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.
    DMA-135 hydrochloride

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