kira6

Catalog No.S8658

For research use only.

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

CAS No. 1589527-65-0

Selleck's kira6 has been cited by 14 publications

Purity & Quality Control

Choose Selective IRE1 Inhibitors

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

Assay
Methods Test Index PMID
Growth inhibition assay Cell count 29423023
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].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: BALB/c mice
  • Dosages: 10 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 518.53
Formula

C28H25F3N6O

CAS No. 1589527-65-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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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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