Referencia número: HY-19708

KIRA6

31 Cited Publications

Revisión del cliente

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.

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Pureza: 98.75%
No. CAS: 1589527-65-0
Fòrmula: C₂₈H₂₅F₃N₆O
Peso molecular:518.53

Almacenamiento:

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

KIRA6 Chemical Structure

No. CAS: 1589527-65-0

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (31)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC₅₀ of 0.6 µM^[2]. KIRA6 can trigger an apoptotic response^[1].

IC₅₀ & Target

IC50: 0.6 µM (IRE1α RNase kinase)^[2]

In Vitro

KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a K_d 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.

Cell Viability Assay^[1]

Cell Line:

HMC-1.1 cells
Concentration:

10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:

72 hours
Result:

Inhibited cell viability from 30 nM.

Western Blot Analysis^[1]

Cell Line:

HMC-1.1 cells
Concentration:

10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:

1 hours
Result:

Reduced expression of phosphorylated KIT, STAT5 and ERK1/2.

RT-PCR^[2]

Cell Line:

INS-1 IRE1α (WT) cells
Concentration:

1 μM
Incubation Time:

0 hour, 12 hours, 24 hours, 48 hours
Result:

Inhibited Ins1 mRNA expression.

Apoptosis Analysis^[2]

Cell Line:

INS-1 IRE1α (WT) cells
Concentration:

1-10 μM
Incubation Time:

72 hours
Result:

Reduced 1NM-PP1 potentiation of Ins1 apoptosis during ER stress.

In Vivo

KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of random glucose levels over several weeks compared to vehicle, both fed ad lib^[2].
? KIRA6 (intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections) increases both plasma insulin and C-peptide levels, remains insulin-positive islet areas at high level after stopping injections in the Akita Mouse^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Ins2+/Akita mice^[2]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections
Result:

Attenuates b cell functional loss, increased insulin levels.

Chemical Information

No. CAS 1589527-65-0
Appearance Solid
Peso molecular 518.53
Fòrmula C₂₈H₂₅F₃N₆O
Color White to light yellow
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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (31)

All Cell Imaging/StainingWBCell Proliferation/Viability AssayRT-PCR

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Journal Impact Factor

Science

IRE1α-XBP1 signaling in leukocytes controls prostaglandin biosynthesis and pain. [Abstract]

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.
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.
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
Nano Today

April 2022, 101416.
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
Hypertension

2025 Dec 30.
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

MANF regulates neuronal survival and UPR through its ER-located receptor IRE1α. [Abstract]

2023 Feb 3;42(2):112066. PMID: 36739529
Int J Mol Sci

IRE1α Is a Therapeutic Target for Cystic Fibrosis Airway Inflammation. [Abstract]

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
University of Pennsylvania

2025.
bioRxiv

GABRA1 frameshift variants impair GABAA receptor proteostasis. [Abstract]

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
University of Oklahoma

2024.

Solvente y solubilidad

In Vitro:

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)

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

1.9285 mL

9.6426 mL

19.2853 mL

5 mM

0.3857 mL

1.9285 mL

3.8571 mL

10 mM

0.1929 mL

0.9643 mL

1.9285 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 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 (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (285 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)
Instrucciones de manejo (2659 KB)

Referencias

[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]

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
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

Keywords

KIRA6

31 Cited Publications

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KIRA6

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Endoplasmic Reticulum Stress Compound 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) KIRA6

Actividad biológica

Chemical Information

Publications (31)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

KIRA6

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-diabetic Compound Library

Endoplasmic Reticulum Stress Compound 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) KIRA6

Actividad biológica

Chemical Information

Publications (31)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

KIRA6 Related Classifications

HY-19708 Related Classifications