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Catalog No. Product Name Information Product Use Citations Product Validations
S7781 Sunitinib 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.
Cell Rep Med, 2024, S2666-3791(24)00201-5
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
S1042 Sunitinib malate 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.
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Pharmaceuticals (Basel), 2024, 17(1)108
Cell Cycle, 2024, 1-13.
S7272 4μ8C 4μ8C (IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
Autophagy, 2024, 1-22.
Cells, 2024, 13(6)527
iScience, 2024, 27(8):110598
S7771 STF-083010 STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Cell Death Dis, 2024, 15(1):31
Cells, 2024, 13(6)527
J Biol Chem, 2024, 300(6):107394
S8658 kira6 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.
iScience, 2024, 27(7):110196
Brain Res, 2024, 1838:149011
Cell Rep Med, 2023, S2666-3791(23)00373-7
S8286 MKC-3946 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.
PLoS One, 2024, 19(6):e0304914
Nat Commun, 2023, 14(1):2132
Int J Biol Sci, 2022, 18(3):1053-1064
S8875 MKC8866 MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro.
EMBO Rep, 2024, 25(4):1792-1813
EMBO Rep, 2022, e51679
iScience, 2022, 25(1):103709
S6623 APY29 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).
Exp Mol Med, 2022, 54(11):1927-1939
E2652 Kira8 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.
Cancer Commun (Lond), 2024, 10.1002/cac2.12583
Stem Cell Reports, 2024, S2213-6711(24)00006-7
bioRxiv, 2023, 2023.06.07.544081
S9797 IXA4 IXA4, a highly selective, non-toxic IRE1/XBP1s activator, activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways, and reduces secretion of amyloid precursor protein (APP) through IRE1 activation, preventing APP-associated mitochondrial dysfunction.
EMBO J, 2023, e113118.
S6495 6-Bromo-2-hydroxy-3-methoxybenzaldehyde 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is a bromobenzaldehyde derivative that participates in the synthesis of (±)-norannuradhapurine. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an IRE-1α inhibitor with an IC50 of 0.08 μM.
S7781 Sunitinib 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.
Cell Rep Med, 2024, S2666-3791(24)00201-5
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
S1042 Sunitinib malate 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.
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
Pharmaceuticals (Basel), 2024, 17(1)108
Cell Cycle, 2024, 1-13.
S7272 4μ8C 4μ8C (IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
Autophagy, 2024, 1-22.
Cells, 2024, 13(6)527
iScience, 2024, 27(8):110598
S7771 STF-083010 STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Cell Death Dis, 2024, 15(1):31
Cells, 2024, 13(6)527
J Biol Chem, 2024, 300(6):107394
S8658 kira6 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.
iScience, 2024, 27(7):110196
Brain Res, 2024, 1838:149011
Cell Rep Med, 2023, S2666-3791(23)00373-7
S8286 MKC-3946 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.
PLoS One, 2024, 19(6):e0304914
Nat Commun, 2023, 14(1):2132
Int J Biol Sci, 2022, 18(3):1053-1064
S8875 MKC8866 MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro.
EMBO Rep, 2024, 25(4):1792-1813
EMBO Rep, 2022, e51679
iScience, 2022, 25(1):103709
S6623 APY29 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).
Exp Mol Med, 2022, 54(11):1927-1939
E2652 Kira8 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.
Cancer Commun (Lond), 2024, 10.1002/cac2.12583
Stem Cell Reports, 2024, S2213-6711(24)00006-7
bioRxiv, 2023, 2023.06.07.544081
S6495 6-Bromo-2-hydroxy-3-methoxybenzaldehyde 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is a bromobenzaldehyde derivative that participates in the synthesis of (±)-norannuradhapurine. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an IRE-1α inhibitor with an IC50 of 0.08 μM.
S9797 IXA4 IXA4, a highly selective, non-toxic IRE1/XBP1s activator, activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways, and reduces secretion of amyloid precursor protein (APP) through IRE1 activation, preventing APP-associated mitochondrial dysfunction.
EMBO J, 2023, e113118.

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Tags: IRE1 inhibitor | IRE1 modulator | IRE1 stress