Art. -Nr.: HY-114368

Kira8

(Synonyms: AMG-18)

14 Cited Publications

Kundenbewertung

Based on 14 publication(s) in Google Scholar

Kira8 (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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Reinheit: 98.90%
CAS. Nr.: 1630086-20-2
Formel: C₃₁H₂₉ClN₆O₃S
Molecular Weight:601.12

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Kira8 Chemical Structure

CAS. Nr.: 1630086-20-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

IRE1α^[1]
IC50: 5.9 nM (IRE1α RNase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-1080	IC₅₀	0.099 μM Compound: 18	Inhibition of human XBP1 splicing in human HT1080-CMV-XBP1-Luciferase cells assessed as luciferase signal by Promega Bright-Glo luciferase assay Inhibition of human XBP1 splicing in human HT1080-CMV-XBP1-Luciferase cells assessed as luciferase signal by Promega Bright-Glo luciferase assay	[PMID: 25589933]

In Vitro

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.

In Vivo

Male Ins2^+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks^[1].
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.

Animal Model:

Male Ins2^+/Akita mice^[1]
Dosage:

50 mg/kg
Administration:

Injected i.p.; daily; for 35 days
Result:

Significant reduction of hyperglycemia became apparent over several weeks.

Chemical Information

CAS. Nr. 1630086-20-2
Appearance Solid
Molecular Weight 601.12
Formel C₃₁H₂₉ClN₆O₃S
Color Off-white to yellow
SMILES

O=S(C1=CC=CC=C1Cl)(NC2=C3C=CC(C)=C(OC4=NC=CC=C4C5=NC(N[C@@H]6CNCCC6)=NC=C5)C3=CC=C2)=O
Synonyms

AMG-18
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (14)

All WBCell Imaging/StainingBio/Physico-chemical Assay

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Journal Impact Factor

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 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 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).
Cell Mol Biol Lett

BIP orchestrates bidirectional ER protein trafficking via co-chaperone complexes. [Abstract]

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 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 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 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.
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
bioRxiv

2026 Jan 13.
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
University of Oklahoma

2024.
bioRxiv

2020 Apr.

Lösungsmittel & Löslichkeit

In Vitro:

Ethanol : 76.92 mg/mL (127.96 mM; ultrasonic and adjust pH to 5 with HCl)

DMSO : 65 mg/mL (108.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 30 mg/mL (49.91 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6636 mL

8.3178 mL

16.6356 mL

5 mM

0.3327 mL

1.6636 mL

3.3271 mL

10 mM

0.1664 mL

0.8318 mL

1.6636 mL

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 4 mg/mL (6.65 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 4 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 3% Ethanol 7% Tween-80 90% Saline

Solubility: ≥ 2.31 mg/mL (3.84 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.17 mg/mL (3.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.17 mg/mL (3.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (8.32 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO / Ethanol	1 mM	1.6636 mL	8.3178 mL	16.6356 mL	41.5890 mL
	5 mM	0.3327 mL	1.6636 mL	3.3271 mL	8.3178 mL
	10 mM	0.1664 mL	0.8318 mL	1.6636 mL	4.1589 mL
	15 mM	0.1109 mL	0.5545 mL	1.1090 mL	2.7726 mL
	20 mM	0.0832 mL	0.4159 mL	0.8318 mL	2.0795 mL
	25 mM	0.0665 mL	0.3327 mL	0.6654 mL	1.6636 mL
	30 mM	0.0555 mL	0.2773 mL	0.5545 mL	1.3863 mL
	40 mM	0.0416 mL	0.2079 mL	0.4159 mL	1.0397 mL
DMSO / Ethanol	50 mM	0.0333 mL	0.1664 mL	0.3327 mL	0.8318 mL
	60 mM	0.0277 mL	0.1386 mL	0.2773 mL	0.6932 mL
	80 mM	0.0208 mL	0.1040 mL	0.2079 mL	0.5199 mL
	100 mM	0.0166 mL	0.0832 mL	0.1664 mL	0.4159 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.

Keywords

Kira8

14 Cited Publications

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Kira8

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Endoplasmic Reticulum Stress Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Kira8

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Kira8

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Endoplasmic Reticulum Stress Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Kira8

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Kira8 Related Classifications

HY-114368 Related Classifications