MKC8866

Catalog No.S8875 Synonyms: IRE1-IN-8866

For research use only.

MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro.

MKC8866 Chemical Structure

CAS No. 1338934-59-0

Selleck's MKC8866 has been cited by 2 Publications

Purity & Quality Control

Choose Selective IRE1 Inhibitors

Biological Activity

Description MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro.
Targets
hIRE1α [1]
(Cell-free assay)
0.29 μM
In vitro

MKC8866 is optimized and refined from a family of IRE1α-specific endoribonuclease inhibitors obtained from a chemical library screen. MKC8866 effectively represses IRE1α-mediated XBP1 splicing in PCa cells and has favorable pharmacokinetic and pharmacodynamic properties.[1]

In vivo

MKC8866 is an IRE1α RNase-specific inhibitor molecule that displays significant therapeutic activity in various preclinical models of PCa in vivo. MKC8866 synergizes with clinical PCa drugs in vivo.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: human PCa cell lines LNCaP and 22Rv1, VCaP cell line, C4-2B cell line
  • Concentrations: 0.2-10 μM
  • Incubation Time: 0.25-24 h
  • Method:

    RNA sequencing. for MKC8866 group, LNCaP cells are treated with either DMSO or 10 μM MKC8866 for 1 day before being induced with 30 nM TG for 3 h.

Animal Research:[1]
  • Animal Models: male nude mice (BALB/c Nu/Nu, 5 weeks of age)
  • Dosages: 200 mg/kg, 300 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 361.35
Formula

C18H19NO7

CAS No. 1338934-59-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=O)OC2=C(C(=C(C=C12)OC)O)C=O)CC(=O)N3CCOCC3

In vivo Formulation Calculator (Clear solution)

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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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Molarity Calculator

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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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