| S7272 |
4μ8C
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4μ8C (IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
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J Integr Plant Biol, 2025, 67(9):2388-2400.
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J Integr Plant Biol, 2025, 10.1111/jipb.13963
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Cancer Lett, 2025, 633:217993
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| S7771 |
STF-083010
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STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
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J Neuroinflammation, 2025, 22(1):38
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Cell Stress Chaperones, 2025, S1355-8145(25)00010-0
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Cell Death Dis, 2024, 15(8):587
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| S8658 |
kira6
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kira6 is a potent type II IRE1α kinase inhibitor with an IC50 of 0.6 μM. It dose-dependently inhibits IRE1α(WT) kinase activity, XBP1 RNA cleavage, Ins2 RNA cleavage and oligomerization.
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J Transl Med, 2025, 23(1):860
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Sci Adv, 2025, 11(8):eadu3011
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J Clin Invest, 2024, 135(1)e179874
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| S8286 |
MKC-3946
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MKC3946 is a potent and soluble IRE1α endoribonuclease domain inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells.
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PLoS One, 2024, 19(6):e0304914
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Nat Commun, 2023, 14(1):2132
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Int J Biol Sci, 2022, 18(3):1053-1064
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| S8875 |
MKC8866
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MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro.
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Cell Commun Signal, 2025, 23(1):217
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EMBO Rep, 2024, 25(4):1792-1813
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EMBO Rep, 2022, e51679
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| E2652 |
Kira8
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Kira8 (Ire-1 inhibitor, 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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Cancer Commun (Lond), 2024, 10.1002/cac2.12583
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Stem Cell Reports, 2024, S2213-6711(24)00006-7
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bioRxiv, 2023, 2023.06.07.544081
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| S6623 |
APY29
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APY29 is a type I kinase inhibitor of IRE1α that binds to the ATP-binding site on IRE1α and inhibits its autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM).
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Exp Mol Med, 2022, 54(11):1927-1939
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| S6495 |
6-Bromo-2-hydroxy-3-methoxybenzaldehyde
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6-Bromo-2-hydroxy-3-methoxybenzaldehyde is a bromobenzaldehyde derivative that participates in the synthesis of (±)-norannuradhapurine. This compound is an IRE-1α inhibitor with an IC50 of 0.08 μM.
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| S7781 |
Sunitinib (SU-11248)
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Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
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Cancer Cell, 2025, 43(4):776-796.e14
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Mol Cancer, 2025, 24(1):179
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J Exp Clin Cancer Res, 2025, 44(1):290
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| S1042 |
Sunitinib (SU11248) Malate
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Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
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Nat Commun, 2025, 16(1):7853
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CNS Neurosci Ther, 2025, 31(12):e70696
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Sci Rep, 2025, 15(1):35889
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