1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. IRE1
  4. IRE1 Inhibitor

IRE1 Inhibitor

IRE1 Inhibitors (33):

Cat. No. Product Name Effect Purity
  • HY-10255A
    Sunitinib
    Inhibitor 98.96%
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2/KDR/Flk-1 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-19707
    4μ8C
    Inhibitor 98.78%
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
  • HY-15845
    STF-083010
    Inhibitor ≥98.0%
    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
  • HY-139214
    IXA4
    Inhibitor 99.16%
    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.
  • HY-104040
    MKC8866
    Inhibitor 99.52%
    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.
  • HY-153475
    IRE1α kinase-IN-9
    Inhibitor
    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).
  • HY-103248
    Toyocamycin
    Inhibitor 99.90%
    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.
  • HY-19708
    KIRA6
    Inhibitor 99.86%
    KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
  • HY-10255
    Sunitinib Malate
    Inhibitor 99.91%
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2/KDR/Flk-1 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-114368
    Kira8
    Inhibitor 99.74%
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-U00459
    GSK2850163
    Inhibitor 98.48%
    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.
  • HY-17537
    APY29
    Inhibitor 99.90%
    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.
  • HY-19710
    MKC3946
    Inhibitor 99.79%
    MKC3946 is a potent IRE1α inhibitor, used for cancer research.
  • HY-107400
    B I09
    Inhibitor 98.82%
    B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
  • HY-136735
    IRE1α kinase-IN-1
    Inhibitor 99.44%
    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).
  • HY-12399
    MKC9989
    Inhibitor 98.33%
    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
  • HY-18509
    IRE1α kinase-IN-2
    Inhibitor 98.50%
    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.
  • HY-153773
    Z4P
    Inhibitor 99.32%
    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).
  • HY-U00460
    3,6-DMAD hydrochloride
    Inhibitor ≥99.0%
    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.
  • HY-124646
    KIRA-7
    Inhibitor 98.33%
    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.