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

MKC8866, un analogue du salicylaldéhyde, est un inhibiteur de IRE1 RNase qui est puissant et sélectif avec un IC50 de 0,29 μM in vitro humaine. MKC8866 inhibe fortement l'expression de la protéine X-box-binding protein 1-spliced (XBP1s) induite par le dithiothréitol avec un EC50 de 0,52 μM et soulage les cellules RPMI 8226 avec un IC50 de 0,14 μM. MKC8866 inhibe la RNase IRE1 dans les cellules cancéreuses du sein, ce qui entraîne une diminution de la production de facteurs pro-tumorigènes et peut inhiber la croissance tumorale du cancer de la prostate (PCa).

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.

For research use only. We do not sell to patients.

MKC8866 Chemical Structure

MKC8866 Chemical Structure

CAS No. : 1338934-59-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 9 publication(s) in Google Scholar

MKC8866 Related Antibodies

Top Publications Citing Use of Products

    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.

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]
    In Vitro

    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 Related Antibodies

    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.
    In Vivo

    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.
    Clinical Trial
    Molecular Weight

    361.35

    Formula

    C18H19NO7
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=CC1=C(O2)C(C(C)=C(CC(N3CCOCC3)=O)C2=O)=CC(OC)=C1O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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
    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.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    Purity & Documentation

    Purity: 99.84%

    COA (249 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References

    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
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    MKC8866 Related Classifications

    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

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