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Catalog No. Product Name Information Product Use Citations Product Validations
E2652New 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.
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) 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.
Clin Cancer Res, 2022, clincanres.4291.2021
NPJ Breast Cancer, 2022, 8(1):44
Cancers (Basel), 2022, 14(7)1639
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.
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).
S7272 4μ8C 4μ8C (IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
Biochem Pharmacol, 2022, 197:114932
EMBO Mol Med, 2021, e14502
Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
S7771 STF-083010 STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Nat Commun, 2022, 13(1):608
Nat Immunol, 2021, 10.1038/s41590-021-01047-4
Int J Mol Sci, 2021, 22(18)9997
S7781 Sunitinib (SU11248) Sunitinib (SU11248) 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.
Blood, 2022, blood.2021014304
Mol Cell, 2022, S1097-2765(22)00105-8
Clin Cancer Res, 2022, clincanres.4291.2021
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.
Cell Rep, 2022, 38(10):110490
Int J Biol Sci, 2022, 18(3):1053-1064
J Immunol, 2020, 204(12):3236-3247
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.
J Dairy Sci, 2022, 105(8):6895-6908
Biometals, 2022, 10.1007/s10534-022-00376-7
Toxicol Res (Camb), 2022, 11(3):498-510
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, 2022, e51679
Front Oncol, 2021, 11:671141
S9797New 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.
E2652New 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.
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) 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.
Clin Cancer Res, 2022, clincanres.4291.2021
NPJ Breast Cancer, 2022, 8(1):44
Cancers (Basel), 2022, 14(7)1639
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.
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).
S7272 4μ8C 4μ8C (IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
Biochem Pharmacol, 2022, 197:114932
EMBO Mol Med, 2021, e14502
Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
S7771 STF-083010 STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Nat Commun, 2022, 13(1):608
Nat Immunol, 2021, 10.1038/s41590-021-01047-4
Int J Mol Sci, 2021, 22(18)9997
S7781 Sunitinib (SU11248) Sunitinib (SU11248) 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.
Blood, 2022, blood.2021014304
Mol Cell, 2022, S1097-2765(22)00105-8
Clin Cancer Res, 2022, clincanres.4291.2021
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.
Cell Rep, 2022, 38(10):110490
Int J Biol Sci, 2022, 18(3):1053-1064
J Immunol, 2020, 204(12):3236-3247
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.
J Dairy Sci, 2022, 105(8):6895-6908
Biometals, 2022, 10.1007/s10534-022-00376-7
Toxicol Res (Camb), 2022, 11(3):498-510
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, 2022, e51679
Front Oncol, 2021, 11:671141
S9797New 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.
E2652New 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.
S9797New 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.
Tags: IRE1 inhibitor | IRE1 modulator | IRE1 stress