MKC8866

製品コードS8875 バッチS887501

印刷

化学情報

Synonyms

IRE1-IN-8866

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₈H₁₉NO₇

分子量

361.35

CAS No.

1338934-59-0

Solubility (25°C)*

体外

DMSO

3 mg/mL (8.3 mM)

Water

˂1 mg/mL

Ethanol

˂1 mg/mL

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.150mg/ml (0.42mM)	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.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.150mg/ml (0.42mM)	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.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro.
in vitro	MKC8866 is optimized and refined from a family of IRE1α-specific endoribonuclease inhibitors obtained from a chemical library screen. This compound 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. This compound synergizes with clinical PCa drugs in vivo.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	human PCa cell lines LNCaP and 22Rv1, VCaP cell line, C4-2B cell line
	濃度	0.2-10 μM
	反応時間	0.25-24 h
	実験の流れ	RNA sequencing. for this compound group, LNCaP cells are treated with either DMSO or 10 μM this chemical for 1 day before being induced with 30 nM TG for 3 h.
動物実験	動物モデル	male nude mice (BALB/c Nu/Nu, 5 weeks of age)
	投薬量	200 mg/kg, 300 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/30679434/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Accumulation of long-chain unsaturated fatty acids in the airway inflammatory microenvironment drives eosinophil etosis and corticosteroid resistance [ Cell Commun Signal, 2025, 23(1):217]	PubMed: 40336088
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。