KIRA6
Based on 31 publication(s) in Google Scholar
KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.75%
- CAS No.: 1589527-65-0
- Formule: C28H25F3N6O
- Masse moléculaire:518.53
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) KIRA6
More- Science. 2019 Jul 19;365(6450):eaau6499. [Abstract]
- ACS Nano. 2021 Sep 28;15(9):14522-14534. [Abstract]
- Nat Commun. 2024 Jan 2;15(1):72. [Abstract]
- Biomaterials. 2026 Aug:331:124089. [Abstract]
- Biomaterials. 2021 May:272:120757. [Abstract]
- J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]
- Redox Biol. 2026 Jun 11:95:104255. [Abstract]
- J Control Release. 2022 Sep:349:254-268. [Abstract]
- Gut Microbes. 2024 Jan-Dec;16(1):2392877. [Abstract]
- Nano Today. April 2022, 101416.
- ACS Cent Sci. 2020 Jan 22;6(1):76-82. [Abstract]
- Cell Mol Biol Lett. 2025 May 14;30(1):59. [Abstract]
- Cell Death Dis. 2023 Aug 26;14(8):561. [Abstract]
- Free Radic Biol Med. 2026 Aug 1:251:440-453. [Abstract]
- Hypertension. 2025 Dec 30.
- Free Radic Biol Med. 2025 Aug 16:236:17-27. [Abstract]
- Free Radic Biol Med. 2025 Jun:233:148-161. [Abstract]
- Br J Pharmacol. 2024 Oct;181(19):3610-3626. [Abstract]
- Int Endod J. 2025 Jul 30. [Abstract]
- Cell Rep. 2023 Feb 3;42(2):112066. [Abstract]
- Int J Mol Sci. 2021 Mar 17;22(6):3063. [Abstract]
- J Inflamm. 2023 Nov 1;20(1):36. [Abstract]
- J Biol Chem. 2022 Jun;298(6):101997. [Abstract]
- Fish Shellfish Immunol. 2020 Mar;98:112-121. [Abstract]
- BMC Oral Health. 2023 Dec 21;23(1):1032. [Abstract]
- Mol Biol Rep. 2022 Oct;49(10):9181-9194. [Abstract]
- FASEB Bioadv. 2025 Jul 9;7(7):e70031. [Abstract]
- University of Pennsylvania. 2025.
- bioRxiv. 2025 Jan 8:2024.11.28.625971. [Abstract]
- bioRxiv. 2024 Aug 8:2024.08.08.607189. [Abstract]
- University of Oklahoma. 2024.
Customer Validation & Images
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RT-PCR
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WB
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RT-PCR
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Cell Imaging/Staining
Activité biologique
IC50: 0.6 µM (IRE1α RNase kinase)[2]
KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a Kd value of 10.8 ?μM[1].? KIRA6 (10-1000 nM; 72 hours) strongly compromises the viability of the KIT-dependent cell line HMC-1.1 at the low nM concentration, in a manner that coincided with KIT blockade[1].? KIRA6 (10-1000 nM; 1 hour) reduces signaling output of KIT,? including the phosphorylation of KIT as well as its downstream signaling modules, PSTAT5 and phosphorylated ERK1/2[1].? KIRA6 (1 μM; 0-48 hours) inhibits Ins1 mRNA decay from IRE1α hyperactivation at a dose-dependent manner[2].? KIRA6 (0.1-10μM; 72 hours) dose-dependently reduces 1NM-PP1 potentiation of Ins1 apoptosis during ER stress in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HMC-1.1 cells
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Concentration:10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
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Incubation Time:72 hours
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Result:Inhibited cell viability from 30 nM.
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Cell Line:HMC-1.1 cells
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Concentration:10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
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Incubation Time:1 hours
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Result:Reduced expression of phosphorylated KIT, STAT5 and ERK1/2.
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Cell Line:INS-1 IRE1α (WT) cells
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Concentration:1 μM
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Incubation Time:0 hour, 12 hours, 24 hours, 48 hours
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Result:Inhibited Ins1 mRNA expression.
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Cell Line:INS-1 IRE1α (WT) cells
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Concentration:1-10 μM
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Incubation Time:72 hours
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Result:Reduced 1NM-PP1 potentiation of Ins1 apoptosis during ER stress.
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[2]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections
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Result:Attenuates b cell functional loss, increased insulin levels.
Chemical Information
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CAS No. 1589527-65-0
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Appearance Solid
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Masse moléculaire 518.53
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Formule C28H25F3N6O
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Color White to light yellow
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SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=C3C=CC=CC3=C(C4=C5C(N)=NC=CN5C(C(C)(C)C)=N4)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (31)
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Journal Impact Factor
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Most Recent
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Science
2019 Jul 19;365(6450):eaau6499. PMID: 31320508 -
ACS Nano
Dual Inhibition of Endoplasmic Reticulum Stress and Oxidation Stress Manipulates the Polarization of Macrophages under Hypoxia to Sensitize Immunotherapy. [Abstract]2021 Sep 28;15(9):14522-14534. PMID: 34414762 -
Nat Commun
A nanoemulsion targeting adipose hypertrophy and hyperplasia shows anti-obesity efficiency in female mice. [Abstract]2024 Jan 2;15(1):72. PMID: 38167723 -
Biomaterials
A translational systems medicine approach to devising nanotherapeutics for targeted intervention of MASLD. [Abstract]2026 Aug:331:124089. PMID: 41762518 -
Biomaterials
Targeted regulation of lymphocytic ER stress response with an overall immunosuppression to alleviate allograft rejection. [Abstract]2021 May:272:120757. PMID: 33798960
KIRA6 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 May:272:120757. [Abstract]
KIRA6 (1.5 μM). TEM images of different liposomes. Scale bar, 100 nm.
KIRA6 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 May:272:120757. [Abstract]
KIRA6 (0.5-15 μM). Cell viability of quiescent (naive) or activated (ɑ-CD3/28 Abs stimulation) splenic T-8 incubated with different liposomes at varying drug concentration for 24 h, respectively, n = 5.
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J Nanobiotechnology
Biomimetic mesenchymal stem cell membrane-coated nanoparticle delivery of MKP5 inhibits hepatic fibrosis through the IRE/XBP1 pathway. [Abstract]2024 Nov 28;22(1):741. PMID: 39609656
KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]
LX-2 cells were pre-treated with Kira6 (0.5 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h, V: Veh, K: Kira6, T: TGF-β1, K + T: Kira6 + TGF-β1. The levels of p-IRE1α and fibrosis-associated proteins were measured using western blotting.
KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]
LX-2 cells were pre-treated with Kira6 (0.5 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h, V: Veh, K: Kira6, T: TGF-β1, K + T: Kira6 + TGF-β1. The mRNA levels of XBP1s.
KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]
AML12 cells were pre-treated with Kira6 (1 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h. The levels of EMT-related proteins were detected using western blotting.
KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]
AML12 cells were pre-treated with Kira6 (1 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h. The mRNA levels of IL-6, IL-1β, TNF-α, and MCP-1 were measured by real-time PCR.
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Redox Biol
TRPV4 drives macrophage pyroptosis via mitochondrial dysfunction and mtROS-dependent NLRP3 inflammasome activation in acute lung injury. [Abstract]2026 Jun 11:95:104255. PMID: 42314332 -
J Control Release
A therapeutic DC vaccine with maintained immunological activity exhibits robust anti-tumor efficacy. [Abstract]2022 Sep:349:254-268. PMID: 35803328 -
Gut Microbes
Bacterial amyloid curli activates the host unfolded protein response via IRE1α in the presence of HLA-B27. [Abstract]2024 Jan-Dec;16(1):2392877. PMID: 39189642 -
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ACS Cent Sci
Direct Quantification of Damaged Nucleotides in Oligonucleotides Using an Aerolysin Single Molecule Interface. [Abstract]2020 Jan 22;6(1):76-82. PMID: 31989027 -
Cell Mol Biol Lett
Narciclasine enhances cisplatin-induced apoptotic cell death by inducing unfolded protein response-mediated regulation of NOXA and MCL1. [Abstract]2025 May 14;30(1):59. PMID: 40369444 -
Cell Death Dis
Targeted inhibition of protein synthesis renders cancer cells vulnerable to apoptosis by unfolded protein response. [Abstract]2023 Aug 26;14(8):561. PMID: 37626037 -
Free Radic Biol Med
Advanced oxidation protein products exacerbate osteoarthritis progression by disrupting stress granules assembly via endoplasmic reticulum stress. [Abstract]2026 Aug 1:251:440-453. PMID: 42009145 -
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Free Radic Biol Med
Neutrophil extracellular traps induce fibroblast ferroptosis via IRE1α/XBP1-mediated ER stress to impair diabetic wound healing. [Abstract]2025 Aug 16:236:17-27. PMID: 40379156 -
Free Radic Biol Med
Autophagy and Endoplasmic Reticulum Stress-Related Protein Homeostasis Links Palmitic Acid to Hepatic Lipotoxicity in Zebrafish (Danio rerio), Counteracted by Linoleic Acid. [Abstract]2025 Jun:233:148-161. PMID: 40089081 -
Br J Pharmacol
Insulin-degrading enzyme inhibition increases the unfolded protein response and favours lipid accumulation in the liver. [Abstract]2024 Oct;181(19):3610-3626. PMID: 38812293 -
Int Endod J
Endoplasmic Reticulum Stress Inhibits the Neuronal Differentiation of Human Stem Cells From Apical Papillae by Attenuating the Activity of ERK-IRE1α Axis In Vitro. [Abstract]2025 Jul 30. PMID: 40739653 -
Cell Rep
2023 Feb 3;42(2):112066. PMID: 36739529 -
Int J Mol Sci
2021 Mar 17;22(6):3063. PMID: 33802742 -
J Inflamm
Soluble epoxide hydrolase deficiency attenuates airway inflammation in COPD via IRE1α/JNK/AP-1 signaling pathway. [Abstract]2023 Nov 1;20(1):36. PMID: 37915073 -
J Biol Chem
Phosphorylation at Ser724 of the ER stress sensor IRE1α governs its activation state and limits ER stress-induced hepatosteatosis. [Abstract]2022 Jun;298(6):101997. PMID: 35500653 -
Fish Shellfish Immunol
Molecular cloning and the involvement of IRE1α-XBP1s signaling pathway in palmitic acid induced - Inflammation in primary hepatocytes from large yellow croaker (Larimichthys crocea). [Abstract]2020 Mar;98:112-121. PMID: 31904542 -
BMC Oral Health
Experimental periodontitis induced hypoadiponectinemia by IRE1α-mediated endoplasmic reticulum stress in adipocytes. [Abstract]2023 Dec 21;23(1):1032. PMID: 38129878 -
Mol Biol Rep
TMBIM6 promotes diabetic tubular epithelial cell survival and albumin endocytosis by inhibiting the endoplasmic reticulum stress sensor, IRE1α. [Abstract]2022 Oct;49(10):9181-9194. PMID: 35857174 -
FASEB Bioadv
Endoplasmic Reticulum Stress and Unfolded Protein Response Sensor ERN1 Regulates Organic Dust Induction of Lung Inflammation. [Abstract]2025 Jul 9;7(7):e70031. PMID: 40641847 -
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bioRxiv
2025 Jan 8:2024.11.28.625971. PMID: 39651292 -
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 -
Solvant et solubilité
DMSO : 25 mg/mL (48.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (285 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[1]. Mahameed M,et al. The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis. 2019 Apr 1;10(4):300. [Content Brief]
[2]. Ghosh R, et al. Allosteric inhibition of the IRE1α RNase preserves cell viability and function during endoplasmic reticulum stress. Cell. 2014 Jul 31;158(3):534-48. [Content Brief]
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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9285 mL | 9.6426 mL | 19.2853 mL | 48.2132 mL |
| 5 mM | 0.3857 mL | 1.9285 mL | 3.8571 mL | 9.6426 mL | |
| 10 mM | 0.1929 mL | 0.9643 mL | 1.9285 mL | 4.8213 mL | |
| 15 mM | 0.1286 mL | 0.6428 mL | 1.2857 mL | 3.2142 mL | |
| 20 mM | 0.0964 mL | 0.4821 mL | 0.9643 mL | 2.4107 mL | |
| 25 mM | 0.0771 mL | 0.3857 mL | 0.7714 mL | 1.9285 mL | |
| 30 mM | 0.0643 mL | 0.3214 mL | 0.6428 mL | 1.6071 mL | |
| 40 mM | 0.0482 mL | 0.2411 mL | 0.4821 mL | 1.2053 mL |
KIRA6 Related Classifications
HY-19708 Related Classifications
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