MKC8866
Based on 17 publication(s) in Google Scholar
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.
- Purity: 99.95%
- CAS No.: 1338934-59-0
- Formula: C18H19NO7
- Molecular Weight:361.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MKC8866
More- Science. 2019 Jul 19;365(6450):eaau6499. [Abstract]
- Nat Immunol. 2025 Feb;26(2):200-214. [Abstract]
- Cancer Res. 2025 Apr 28:OF1-OF13. [Abstract]
- Adv Sci (Weinh). 2025 Sep 12:e09588. [Abstract]
- Cell Rep Med. 2026 May 19;7(5):102788. [Abstract]
- J Exp Med. 2022 Nov 7;219(11):e20221085. [Abstract]
- Cancer Lett. 2020 Oct 10;490:76-88. [Abstract]
- Cell Death Dis. 2022 Apr 20;13(4):384. [Abstract]
- Int Endod J. 2025 Jul 30. [Abstract]
- Clin Transl Med. 2024 Nov;14(11):e70082. [Abstract]
- Int J Mol Sci. 2022 Aug 14;23(16):9113. [Abstract]
- Front Pharmacol. 2022 Mar 21;13:854506. [Abstract]
- Front Microbiol. 2025 Sep 3:16:1648467. [Abstract]
- Sci Rep. 2019 Mar 1;9(1):3210. [Abstract]
- Am J Pathol. 2026 Mar 19:S0002-9440(26)00065-9. [Abstract]
- J Diabetes Investig. 2023 Mar;14(3):364-375. [Abstract]
- bioRxiv. 2026 Feb 1:2026.01.28.702376. [Abstract]
Customer Validation & Images
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WB
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RT-PCR
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RT-PCR
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WB
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RT-PCR
Biological Activity
IC50: 0.29 μM (IRE1 RNase)[1]
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.
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Cell Line:MCF7, SKBR3, MDA-MB-231 and MCF10A cells
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Concentration:20 μM
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Incubation Time:For 6 days
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Result:Decreased proliferation of all breast cancer cell lines.
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Cell Line:MDA-MB-231, MCF7 and SKBR3 cells
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Concentration:20 μM
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Incubation Time:48 hours
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Result:Reduced the number of cells entering S phase.
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Cell Line:LNCaP, VCaP, 22Rv1 and C4-2B cells
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Concentration:0.2, 0.5, 1, 5, 10 μM
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Incubation Time:3 days
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Result:Suppressed the viability of all four cell lines in a dose-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:20 μM
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Incubation Time:72 hours
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Result:Completely blocked NSC 125973-induced expression of XBP1s.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice with MDA-MB-231 tumor[1]
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Dosage:300 mg/kg
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Administration:Oral; for 28 days
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Result:Reduced tumor regrowth post-NSC 125973 withdrawal.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1338934-59-0
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Appearance Solid
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Molecular Weight 361.35
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Formula C18H19NO7
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Color Light yellow to yellow
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SMILES
O=CC1=C(O2)C(C(C)=C(CC(N3CCOCC3)=O)C2=O)=CC(OC)=C1O
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Synonyms
Orin1001
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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Journal Impact Factor
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Most Recent
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Science
2019 Jul 19;365(6450):eaau6499. PMID: 31320508 -
Nat Immunol
IRE1α-XBP1 safeguards hematopoietic stem and progenitor cells by restricting pro-leukemogenic gene programs. [Abstract]2025 Feb;26(2):200-214. PMID: 39789376 -
Cancer Res
Blocking the TCA Cycle in Cancer Cells Potentiates CD36+ T-cell-Mediated Antitumor Immunity by Suppressing ER Stress-Associated THBS2 Signaling. [Abstract]2025 Apr 28:OF1-OF13. PMID: 40293258
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.
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Adv Sci (Weinh)
XBP1s Mediates Cross-resistance to Combination Treatment of CDK4/6 Inhibitors plus Endocrine Therapy in Breast Cancer. [Abstract]2025 Sep 12:e09588. PMID: 40940685 -
Cell Rep Med
Taxane chemotherapy promotes response to TIM-3 checkpoint blockade via STING-mediated ER stress and HMGB1 secretion. [Abstract]2026 May 19;7(5):102788. PMID: 42097146 -
J Exp Med
Chronic activation of pDCs in autoimmunity is linked to dysregulated ER stress and metabolic responses. [Abstract]2022 Nov 7;219(11):e20221085. PMID: 36053251
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.
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Cancer Lett
The IRE1 and PERK arms of the unfolded protein response promote survival of rhabdomyosarcoma cells. [Abstract]2020 Oct 10;490:76-88. PMID: 32679165
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.
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Cell Death Dis
Mitochondrial oxidative phosphorylation is dispensable for survival of CD34+ chronic myeloid leukemia stem and progenitor cells. [Abstract]2022 Apr 20;13(4):384. PMID: 35444236 -
Int Endod J
Endoplasmic Reticulum Stress Inhibits the Neuronal Differentiation of Human Stem Cells From Apical Papillae by Attenuating the Activity of ERK-IRE1α Axis In Vitro. [Abstract]2025 Jul 30. PMID: 40739653 -
Clin Transl Med
Targeting endoplasmic reticulum stress-induced lymphatic dysfunction for mitigating bisphosphonate-related osteonecrosis. [Abstract]2024 Nov;14(11):e70082. PMID: 39521624 -
Int J Mol Sci
Concomitant Inhibition of IRE1α/XBP1 Axis of UPR and PARP: A Promising Therapeutic Approach against c-Myc and Gammaherpesvirus-Driven B-Cell Lymphomas. [Abstract]2022 Aug 14;23(16):9113. PMID: 36012375 -
Front Pharmacol
2022 Mar 21;13:854506. PMID: 35387352 -
Front Microbiol
Ire1 inhibitors attenuate Candida albicans pathogenicity and demonstrate potential for application in antifungal therapy. [Abstract]2025 Sep 3:16:1648467. PMID: 40969430 -
Sci Rep
2019 Mar 1;9(1):3210. PMID: 30824833 -
Am J Pathol
R-Propranolol Promotes the Adipogenesis and Subsequent Apoptosis of Hemangioma Stem Cells through the Protein Kinase RNA-Like Endoplasmic Reticulum Kinase Signaling Pathway. [Abstract]2026 Mar 19:S0002-9440(26)00065-9. PMID: 41864339 -
J Diabetes Investig
Sinomenine alleviates diabetic peripheral neuropathic pain through inhibition of the inositol-requiring enzyme 1 alpha-X-box binding protein 1 pathway by downregulating prostaglandin-endoperoxide synthase 2. [Abstract]2023 Mar;14(3):364-375. PMID: 36692011 -
bioRxiv
The active secretion of a subunit of IL-12 by tissue cells is regulated by Valosin-Containing Protein and intracellular calcium redistribution. [Abstract]2026 Feb 1:2026.01.28.702376. PMID: 41659431
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Sheng X, et al. IRE1α-XBP1s pathway promotes prostate cancer by activating c-MYC signaling. Nat Commun. 2019 Jan 24;10(1):323. [Content Brief]
[2]. Logue SE, et al. Inhibition of IRE1 RNase activity modulates the tumor cell secretome and enhances response to chemotherapy. Nat Commun. 2018 Aug 15;9(1):3267. [Content Brief]
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 |
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| 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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