Home ER stress & UPR IRE1 inhibitor kira6 For research use only.

kira6

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 Chemical Structure

kira6 Chemical Structure

CAS No. 1589527-65-0

Purity & Quality Control

kira6 Related Products

Biological Activity

Description 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.
Targets
IRE1α [1]
(Cell-free)
0.6 μM
In vitro
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].
Cell Research Cell lines THP-1 cells
Concentrations 0.5 μM
Incubation Time 4 h
Method

Cells were treated with various concentrations of drug.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell count 29423023
In Vivo
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].
Animal Research Animal Models BALB/c mice
Dosages 10 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 518.53 Formula

C28H25F3N6O
CAS No. 1589527-65-0 SDF --
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 60 mg/mL ( (115.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble


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In vivo
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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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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