Home ER stress & UPR IRE1 inhibitor MKC8866 For research use only.

MKC8866

Synonyms: IRE1-IN-8866

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

MKC8866 Chemical Structure

CAS: 1338934-59-0

Selleck's MKC8866 has been cited by 3 publications

Purity & Quality Control

Batch: S887501 DMSO] 3 mg/mL] false] Water] ˂1 mg/mL] false] Ethanol] ˂1 mg/mL] false Purity: 98.94%
98.94

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models male nude mice (BALB/c Nu/Nu, 5 weeks of age)
Dosages 200 mg/kg, 300 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 361.35 Formula

C18H19NO7
CAS No. 1338934-59-0 SDF --
Smiles CC1=C(C(=O)OC2=C(C(=C(C=C12)OC)O)C=O)CC(=O)N3CCOCC3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 3 mg/mL ( (8.3 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL


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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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