Kira8 Hydrochloride
Based on 14 publication(s) in Google Scholar
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
For research use only. We do not sell to patients.
- Purity: 98.03%
- CAS No.: 2250019-92-0
- Formula: C31H30Cl2N6O3S
- Molecular Weight:637.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Kira8 Hydrochloride
More- Nucleic Acids Res. 2023 May 8;51(8):3650-3670. [Abstract]
- Cell Mol Biol Lett. 2026 Feb 14. [Abstract]
- NPJ Parkinsons Dis. 2023 Mar 7;9(1):35. [Abstract]
- Life Sci. 2026 Jan 1:384:124091. [Abstract]
- Biomed J. 2025 Jun 2:100875. [Abstract]
- Radiother Oncol. 2024 Feb:191:110059. [Abstract]
- Int J Mol Sci. 2022 Aug 12;23(16):9000. [Abstract]
- Am J Physiol Lung Cell Mol Physiol. 2021 Sep 1;321(3):L576-L594. [Abstract]
- Arch Biochem Biophys. 2023 Mar 15:737:109552. [Abstract]
- Biochem Biophys Res Commun. 2022 Sep 29;632:158-164. [Abstract]
- bioRxiv. 2026 Jan 13.
- bioRxiv. 2024 Aug 8:2024.08.08.607189. [Abstract]
- University of Oklahoma. 2024.
- bioRxiv. 2020 Apr.
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WB
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Biological Activity
Kira8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. Kira8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Ins2+/Akita mice[1]
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Dosage:50 mg/kg
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Administration:Injected i.p.; daily; for 35 days
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Result:Significant reduction of hyperglycemia became apparent over several weeks.
Chemical Information
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CAS No. 2250019-92-0
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Appearance Solid
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Molecular Weight 637.58
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Formula C31H30Cl2N6O3S
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Color White to yellow
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SMILES
O=S(C1=CC=CC=C1Cl)(NC2=C3C=CC(C)=C(C3=CC=C2)OC4=NC=CC=C4C5=NC(N[C@H]6CNCCC6)=NC=C5)=O.[H]Cl
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Synonyms
AMG-18 Hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (14)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
Genomic targets of the IRE1-XBP1s pathway in mediating metabolic adaptation in epithelial plasticity. [Abstract]2023 May 8;51(8):3650-3670. PMID: 36772828
Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 May 8;51(8):3650-3670. [Abstract]
FXBP1s expression. Western immunoblot of hSAECs transduced with empty (pCT) or FXBP1s-expressing lentiviral vector at an MOI of 2.0 for 48 h, or mock-treated or treated with tunicamycin (TM, 0.5 μg/ml for 8 h) or thapsigargin (Tg, 50 nM for 6 h) in the absence or presence of KIRA8 (10 μM). Nuclear extracts were prepared and stained with anti-FLAG M2 or anti-XBP1s antibodies. TBP was used as loading control.
Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 May 8;51(8):3650-3670. [Abstract]
We observed that Tg induced a 3.5 ± 0.5-fold increase in endogenous XBP1s binding to the GFPT1 promoter. This induction was completely inhibited by the treatment with KIRA8 (10 μM).
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Cell Mol Biol Lett
2026 Feb 14. PMID: 41691145 -
NPJ Parkinsons Dis
Deficiency of Perry syndrome-associated p150Glued in midbrain dopaminergic neurons leads to progressive neurodegeneration and endoplasmic reticulum abnormalities. [Abstract]2023 Mar 7;9(1):35. PMID: 36879021 -
Life Sci
Inhibition of IRE1α by KIRA8 restores spingosine-1-phosphate lyase activity and improves insulin sensitivity in muscle cells. [Abstract]2026 Jan 1:384:124091. PMID: 41253238 -
Biomed J
IRE1-Mediated Endoplasmic Reticulum Stress Response Regulates Oxidative Damage in CYP4V2 Deficient Human Retinal Pigment Epithelial Cells. [Abstract]2025 Jun 2:100875. PMID: 40466971 -
Radiother Oncol
Identification of the unfolded protein response pathway as target for radiosensitization in pancreatic cancer. [Abstract]2024 Feb:191:110059. PMID: 38135186 -
Int J Mol Sci
The IRE1α-XBP1s Arm of the Unfolded Protein Response Activates N-Glycosylation to Remodel the Subepithelial Basement Membrane in Paramyxovirus Infection. [Abstract]2022 Aug 12;23(16):9000. PMID: 36012265
Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000. [Abstract]
In a manner similar to our observations on the RSV induction of cell-associated FN1, we found that FN1 deposition into the ECM was also blocked by KIRA8 (10 μM, pre-treated for two hours).
Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000. [Abstract]
Principal component analysis of significant proteins (ANOVA with permutation-based FDR < 0.01). Green circle, controls; red square, RSV infection; blue diamond, RSV infection + KIRA8 treatment.
Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000. [Abstract]
Proteomics analysis of N-glycosylation in hSAECs infected with RSV in the presence or absence of KIRA8. hSAECs were infected with RSV at 1.0 MOI for 24 h in the presence or absence of KIRA8 (10 µM). The N-glycosylated peptides were enriched with lectins and then analyzed with label-free LC-MS/MS. Volcano plot of N-glycosylated peptides (RSV vs. Control). Red circle, N-glycoproteins upregulated by RSV; green square, N-glycoproteins downregulated by RSV infection.
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Am J Physiol Lung Cell Mol Physiol
Paramyxovirus replication induces the hexosamine biosynthetic pathway and mesenchymal transition via the IRE1α-XBP1s arm of the unfolded protein response. [Abstract]2021 Sep 1;321(3):L576-L594. PMID: 34318710 -
Arch Biochem Biophys
XBP1s acts as a transcription factor of IRE1α and promotes proliferation of colon cancer cells. [Abstract]2023 Mar 15:737:109552. PMID: 36828260 -
Biochem Biophys Res Commun
KIRA8 attenuates non-alcoholic steatohepatitis through inhibition of the IRE1α/XBP1 signalling pathway. [Abstract]2022 Sep 29;632:158-164. PMID: 36209584 -
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bioRxiv
The mammalian Ire1 inhibitor, 4μ8C, exhibits broad anti- Aspergillus activity in vitro and in a treatment model of fungal keratitis. [Abstract]2024 Aug 8:2024.08.08.607189. PMID: 39149375 -
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Solvent & Solubility
H2O : ≥ 100 mg/mL (156.84 mM)
DMSO : 50 mg/mL (78.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / H2O | 1 mM | 1.5684 mL | 7.8422 mL | 15.6843 mL | 39.2108 mL |
| 5 mM | 0.3137 mL | 1.5684 mL | 3.1369 mL | 7.8422 mL | |
| 10 mM | 0.1568 mL | 0.7842 mL | 1.5684 mL | 3.9211 mL | |
| 15 mM | 0.1046 mL | 0.5228 mL | 1.0456 mL | 2.6141 mL | |
| 20 mM | 0.0784 mL | 0.3921 mL | 0.7842 mL | 1.9605 mL | |
| 25 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5684 mL | |
| 30 mM | 0.0523 mL | 0.2614 mL | 0.5228 mL | 1.3070 mL | |
| 40 mM | 0.0392 mL | 0.1961 mL | 0.3921 mL | 0.9803 mL | |
| 50 mM | 0.0314 mL | 0.1568 mL | 0.3137 mL | 0.7842 mL | |
| 60 mM | 0.0261 mL | 0.1307 mL | 0.2614 mL | 0.6535 mL | |
| H2O | 80 mM | 0.0196 mL | 0.0980 mL | 0.1961 mL | 0.4901 mL |
| 100 mM | 0.0157 mL | 0.0784 mL | 0.1568 mL | 0.3921 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.