The serine/threonine-protein kinase/endoribonuclease inositol-requiring enzyme 1 (IRE1) is an enzyme that in humans is encoded by the ERN1 gene. IRE1 is an endoplasmic reticulum (ER) transmembrane sensor that activates UPR to maintain ER and cellular function. While mammalian IRE1 promotes cell survive, it can initiate apoptosis via decay of anti-apoptotic microRNAs. IRE1 activation is initiated by homotypic interactions of the stress-sensing lumenal domain favoring transautophosphorylation of the kinase-extension nuclease (KEN) domain on the cytoplasmic side of the ER membrane. IRE1/XBP-1 has been shown to regulate a variety of genes in various cell types in response to ER stress, mostly related to ER function and the secretory pathway, although the target genes vary depending on the cell type and nature of the stress stimuli.


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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
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NF-κB >
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Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
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Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

MKC3946

MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.

  • CAS Number: 1093119-54-0
  • MF: C21H20N2O3S
  • MW: 380.460
  • Catalog: IRE1
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 591.6±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 311.6±30.1 °C

4μ8C

4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.

  • CAS Number: 14003-96-4
  • MF: C11H8O4
  • MW: 204.17900
  • Catalog: IRE1
  • Density: 1.406±0.06 g/cm3 (20 ºC 760 Torr)
  • Boiling Point: N/A
  • Melting Point: 189-190 ºC (ethanol )
  • Flash Point: N/A

MKC9989

MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.

  • CAS Number: 1338934-20-5
  • MF: C17H20O7
  • MW: 336.336
  • Catalog: IRE1
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 512.2±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 184.5±23.6 °C

IRE1α kinase-IN-9

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)[1].

  • CAS Number: 1338933-30-4
  • MF: C24H24N2O6
  • MW: 436.46
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRE1α kinase-IN-3

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[1].

  • CAS Number: 2416223-41-9
  • MF: C29H32N6O3S
  • MW: 544.67
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sunitinib malate

Sunitinib Malate (SU 11248 Malate) is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC50s of 80 nM and 2 nM, respectively.

  • CAS Number: 341031-54-7
  • MF: C26H33FN4O7
  • MW: 532.561
  • Catalog: Apoptosis
  • Density: 1.3600 g/mL at 25 °C(lit.)
  • Boiling Point: 156 °C(lit.)
  • Melting Point: 189-191°C
  • Flash Point: 163 °F

Sunitinib D10

Sunitinib D10 (SU 11248 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].

  • CAS Number: 1126721-82-1
  • MF: C22H17D10FN4O2
  • MW: 408.53500
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NSC95682

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.

  • CAS Number: 20035-41-0
  • MF: C8H7BrO3
  • MW: 231.04300
  • Catalog: IRE1
  • Density: 1.653g/cm3
  • Boiling Point: 282.1ºC at 760mmHg
  • Melting Point: 102-105 °C(lit.)
  • Flash Point: 124.4ºC

IXA6

IXA6 is a novel IRE1/XBP1s activator, and can induce IRE1 RNase activity[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

STF-083010

STF-083010 is an Ire1 inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

  • CAS Number: 307543-71-1
  • MF: C15H11NO3S2
  • MW: 317.38300
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sunitinib-d4

Sunitinib-d4 (SU 11248-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].

  • CAS Number: 1126721-79-6
  • MF: C22H23D4FN4O2
  • MW: 402.50
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GSK2850163

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.

  • CAS Number: 2121989-91-9
  • MF: C24H29Cl2N3O
  • MW: 446.41
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

APY 29

APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.

  • CAS Number: 1216665-49-4
  • MF: C17H16N8
  • MW: 332.362
  • Catalog: IRE1
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 782.3±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 426.9±35.7 °C

3,6-DMAD dihydrochloride

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[1][2].

  • CAS Number: 2226511-77-7
  • MF: C22H33Cl2N5
  • MW: 438.44
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRE1α kinase-IN-7

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[1].

  • CAS Number: 1414938-22-9
  • MF: C28H25F3N6O
  • MW: 518.53
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KIRA-7

KIRA-7 is a small molecule inhibitor of IRE1α kinase/Rnase with IC50 of 0.11/0.22 uM, allosterically inhibits IRE1α RNase activity; reverses bleomycin-induced fibrosis when given 2 weeks after bleomycin exposure in vivo.

  • CAS Number: 1937235-76-1
  • MF: C27H23FN6O
  • MW: 466.52
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Toyocamycin

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. Toyocamycin (Vengicide) induces apoptosis. Toyocamycin (Vengicide) shows no effect on IRE1α auto-phosphorylation[1].

  • CAS Number: 606-58-6
  • MF: C12H13N5O4
  • MW: 291.26300
  • Catalog: IRE1
  • Density: 1.91g/cm3
  • Boiling Point: 721.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 389.9ºC

B I09

B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.

  • CAS Number: 1607803-67-7
  • MF: C16H17NO5
  • MW: 303.31
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IRE1α kinase-IN-6

IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.

  • CAS Number: 2715123-88-7
  • MF: C25H23Cl2FN6O3S2
  • MW: 609.52
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Kira8

Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase[1].

  • CAS Number: 1630086-20-2
  • MF: C31H29ClN6O3S
  • MW: 601.12
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IXA4

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[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MKC8866

MKC8866 is an inositol requiring enzyme 1 (IRE-1α) inhibitor with an IC50 of less than 0.1 μM.

  • CAS Number: 1338934-59-0
  • MF: C18H19NO7
  • MW: 361.35
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Kira8 Hydrochloride

Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1].

  • CAS Number: 2250019-92-0
  • MF: C31H30Cl2N6O3S
  • MW: 637.58
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KIRA6

KIRA6 allosterically inhibits IRE1α RNase kinase activity with an IC50 of 0.6 µM.

  • CAS Number: 1589527-65-0
  • MF: C28H25F3N6O
  • MW: 518.533
  • Catalog: IRE1
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A