| Identification | Back Directory | [Name]
MKC8866 | [CAS]
1338934-59-0 | [Synonyms]
181697
MKC8866
MKC8866;MKC-8866
IRE1 RNase inhibitor 8866
IRE1 RNase inhibitor 8866
(MKC8866
7-hydroxy-6-methoxy-4-methyl-3-(2-morpholino-2-oxoethyl)-2-oxo-2H-chromene-8-carbaldehyde
2H-1-Benzopyran-8-carboxaldehyde, 7-hydroxy-6-methoxy-4-methyl-3-[2-(4-morpholinyl)-2-oxoethyl]-2-oxo- | [Molecular Formula]
C18H19NO7 | [MOL File]
1338934-59-0.mol | [Molecular Weight]
361.35 |
| Chemical Properties | Back Directory | [Boiling point ]
620.0±55.0 °C(Predicted) | [density ]
1.373±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:16.67(Max Conc. mg/mL);46.13(Max Conc. mM) | [form ]
A solid | [pka]
6.20±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
MKC8866 (IRE1-IN-8866) is a salicylaldehyde analog, a specific IRE1α RNase inhibitor with IC50 of 0.29 μM against human IRE1α in vitro. | [in vivo]
MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal[1]. | 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.
|
| [target]
| Target | Value | hIRE1α
(Cell-free assay) | 0.29 μM |
| [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. DOI:10.1038/s41467-018-08152-3
[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. DOI:10.1038/s41467-018-05763-8 |
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| Company Name: |
ChemShuttle, Inc.
|
| Tel: |
0510-83588313-811 18800520310 |
| Website: |
https://www.jiehuapharma.com/ |
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