2. Cell Cycle/DNA Damage
  3. IRE1
  4. MKC8866

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1338934-59-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 264 在庫あり
Solution
10 mM * 1 mL in DMSO USD 264 在庫あり
Solid
5 mg $240 在庫あり
10 mg $336 在庫あり
25 mg $570 在庫あり
50 mg $750 在庫あり
100 mg $1020 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 16 publication(s) in Google Scholar

Other Forms of MKC8866:

MKC8866 関連抗体

Top Publications Citing Use of Products

    MKC8866 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Apr 28:OF1-OF13.  [Abstract]

    Effect of ER stress deactivator MKC8866 on TG or CPI-613-induced inhibition of XBP1s and THBS2 expression in HN6 and HN12 cells. Cells were pretreated with 10 μM MKC8866 for 4 hrs before TG or CPI-613 treatment.

    MKC8866 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2022 Nov 7;219(11):e20221085.  [Abstract]

    pDCs from HDs (n = 5) were cultured in medium only, medium with TM, or medium with TG alone or in combination with IRE1α inhibitors (MKC8866 at 1 µM) for 3 h, before addition of the TLR9 agonist. Gene expression levels of IFNA were quantified at 5 h and normalized to TLR9 agonist treatment.

    MKC8866 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2022 Nov 7;219(11):e20221085.  [Abstract]

    pDCs (n = 4) were cultured with TM alone or in combination with an IRE1α inhibitor (MKC8866 at 1 μM) for 8 h. Gene expression level of PHGDH was quantified and normalized to TM treatment.

    MKC8866 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2020 Oct 10;490:76-88.  [Abstract]

    RH30 and RD cells are treated with MKC8866 (20 μM) and/or AMGEN44 (2 μM) for 72 hours and Western blot confirmes IRE1 and PERK signalling inhibition. In cells treated with AMGEN44 alone or in combination with MKC8866, PERK phosphorylation is reduced and p-eIF2α protein levels are diminished. In cells treated with MKC8866 alone or in combination with AMGEN44, XBP1s protein levels are completely abolished.

    MKC8866 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2020 Oct 10;490:76-88.  [Abstract]

    IRE1 signalling was assessed by measuring XBP1 splicing. Untreated and MKC8866- (20 μM) treated RMS cells were collected at 72 h and XBP1s mRNA levels were examined using RT-PCR. GAPDH was used as a loading control.

    MKC8866 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2020 Oct 10;490:76-88.  [Abstract]

    RH30 and RD cells were treated with MKC8866 (20 μM) and/or AMGEN44 (2 μM) for 72 h. Cell viability was assessed using CTG and is expressed as the percentage of untreated controls.

    MKC8866 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2020 Oct 10;490:76-88.  [Abstract]

    For proliferation and senescence assays, cells were treated with MKC8866 (20 μM) and AMGEN44 single and combination treatments for 6 days (treatment was reapplied at 72 h). RH30-miR-146-GFP and RD-miR-146-GFP-treated cells were stained with Hoechst-3342, and fluorescence of GFP and DAPI was measured, imaged and analysed using a MetaXpress microscope. DAPI-FITC overlay images were generated; Blue: DAPI-stained nuclei, Green: GFP- positive cells.

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM[1]. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth[2].

    IC50 & Target

    IC50: 0.29 μM (IRE1 RNase)[1]
    体外実験

    MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines[2].
    MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase[2].
    MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells[1].
    MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s [1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    MKC8866 関連抗体

    Cell Proliferation Assay[2]

    Cell Line: MCF7, SKBR3, MDA-MB-231 and MCF10A cells
    Concentration: 20 μM
    Incubation Time: For 6 days
    Result: Decreased proliferation of all breast cancer cell lines.

    Cell Cycle Analysis[2]

    Cell Line: MDA-MB-231, MCF7 and SKBR3 cells
    Concentration: 20 μM
    Incubation Time: 48 hours
    Result: Reduced the number of cells entering S phase.

    Cell Cycle Analysis[1]

    Cell Line: LNCaP, VCaP, 22Rv1 and C4-2B cells
    Concentration: 0.2, 0.5, 1, 5, 10 μM
    Incubation Time: 3 days
    Result: Suppressed the viability of all four cell lines in a dose-dependent manner.

    Cell Cycle Analysis[2]

    Cell Line: MDA-MB-231 cells
    Concentration: 20 μM
    Incubation Time: 72  hours
    Result: Completely blocked NSC 125973-induced expression of XBP1s.
    体内実験

    MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female athymic nude mice with MDA-MB-231 tumor[1]
    Dosage: 300 mg/kg
    Administration: Oral; for 28 days
    Result: Reduced tumor regrowth post-NSC 125973 withdrawal.
    臨床実験
    分子量

    361.35

    分子式

    C18H19NO7
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=CC1=C(O2)C(C(C)=C(CC(N3CCOCC3)=O)C2=O)=CC(OC)=C1O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 6.67 mg/mL (18.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7674 mL 13.8370 mL 27.6740 mL
    5 mM 0.5535 mL 2.7674 mL 5.5348 mL
    10 mM 0.2767 mL 1.3837 mL 2.7674 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  15% Solutol HS 15    10% Cremophor EL    35% PEG400    40% Water

      Solubility: 20 mg/mL (55.35 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    純度とドキュメンテーション

    純度: 99.95%

    COA (250 KB) HNMR (112 KB) RP-HPLC (249 KB) MS (110 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7674 mL 13.8370 mL 27.6740 mL 69.1850 mL
    5 mM 0.5535 mL 2.7674 mL 5.5348 mL 13.8370 mL
    10 mM 0.2767 mL 1.3837 mL 2.7674 mL 6.9185 mL
    15 mM 0.1845 mL 0.9225 mL 1.8449 mL 4.6123 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    MKC8866 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    MKC88661338934-59-0Orin1001MKC 8866MKC-8866Orin 1001Orin-1001IRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    カスタマ需要量 *

    お名前 *

    		 

    タイトル

    メールアドレス *

    		 

    電話番号 *

    デパートメント

    		 

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    MKC8866
    製品番号:
    HY-104040
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    メールアドレス *

    電話番号 *

    		 

    部門 *

    組纖名 *

    		 

    国或いは地域 *

    備考

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.