MKC8866

Catalog No.S8875 Batch:S887501

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Technical Data

Formula

C18H19NO7
Molecular Weight 361.35 CAS No. 1338934-59-0
Solubility (25°C)* In vitro DMSO 3 mg/mL (8.3 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.15mg/ml Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.15mg/ml Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:[1]
  • Animal Models

    male nude mice (BALB/c Nu/Nu, 5 weeks of age)

  • Dosages

    200 mg/kg, 300 mg/kg

  • Administration

    Oral gavage

Selleck's MKC8866 has been cited by 5 publications

IRE1 RNase controls CD95-mediated cell death [ EMBO Rep, 2024, 25(4):1792-1813] PubMed: 38383861
EI24 promotes cell adaption to ER stress by coordinating IRE1 signaling and calcium homeostasis [ EMBO Rep, 2022, e51679] PubMed: 35005829
Clusterin is involved in mediating the metabolic function of adipose SIRT1 [ iScience, 2022, 25(1):103709] PubMed: 35072003
Clusterin is involved in mediating the metabolic function of adipose SIRT1 [ iScience, 2022, 25(1):103709] PubMed: 35072003
IRE1α Expedites the Progression of Castration-Resistant Prostate Cancers via the Positive Feedback Loop of IRE1α/IL-6/AR [ Front Oncol, 2021, 11:671141] PubMed: 34295814

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.