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kira6 IRE1 inhibitor

Cat.No.S8658

kira6 is a potent type II IRE1α kinase inhibitor with an IC50 of 0.6 μM. It dose-dependently inhibits IRE1α(WT) kinase activity, XBP1 RNA cleavage, Ins2 RNA cleavage and oligomerization.
kira6 IRE1 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 518.53

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 518.53 Formula

C28H25F3N6O

 Storage (From the date of receipt)
CAS No. 1589527-65-0 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)(C)C1=NC(=C2N1C=CN=C2N)C3=CC=C(C4=CC=CC=C43)NC(=O)NC5=CC=CC(=C5)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (115.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
IRE1α [1]
(Cell-free)
0.6 μM
In vitro

In INS-1 cells, KIRA6 inhibits IRE1α auto-phosphorylation by Tg and XBP1 mRNA splicing by Tm in a dose-dependent manner[1].
In vivo

Intravitreally, KIRA6 preserves photoreceptor functional viability in rat models of ER stress-induced retinal degeneration. Systemically, KIRA6 preserves pancreatic β-cells, increases insulin, and reduces hyperglycemia in Akita diabetic mice. KIRA6 inhibits IRE1α in vivo to preserve cell viability and function in diverse cells and rodent tissues experiencing ER stress. The pharmacokinetic profile of KIRA6 in BALB/c mice intraperitoneally (i.p.) dosed at 10 mg/kg shows good drug plasma AUC levels (AUC 0-24h = 14.3 μM*h) with moderate clearance (22.4 mL/min/kg). Drug half-life is 3.90 hours, Cmax is 3.3 μM, and plasma levels at 4 and 8hr are 1.2 μM and 0.33 μM, respectively[1].
References

Applications

Methods Biomarkers Images PMID
Growth inhibition assay Cell count S8658-viability1 29423023

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