MKC8866
- Product Name
- MKC8866
- CAS No.
- 1338934-59-0
- Chemical Name
- MKC8866
- Synonyms
- 181697;MKC8866;MKC8866;MKC-8866;IRE-1α inhibitor 1;MKC8866, 10 mM in DMSO;IRE1 RNase inhibitor 8866;IRE1 RNase inhibitor 8866 (MKC8866;Inositol requiring enzyme 1,inhibit,MKC-8866,IRE1,MKC8866,Inhibitor,MKC 8866;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-
- CBNumber
- CB44796671
- Molecular Formula
- C18H19NO7
- Formula Weight
- 361.35
- MOL File
- 1338934-59-0.mol
MKC8866 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- Axon3223
- Product name
- MKC8866
- Purity
- 99%
- Packaging
- 5mg
- Price
- $115.5
- Updated
- 2021/12/16
- Product number
- Axon3223
- Product name
- MKC8866
- Purity
- 99%
- Packaging
- 25mg
- Price
- $401.5
- Updated
- 2021/12/16
- Product number
- CS-0026810
- Product name
- MKC8866
- Purity
- 99.87%
- Packaging
- 5mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- Axon3223
- Product name
- MKC8866
- Purity
- 99%
- Packaging
- 2x25mg
- Price
- $616
- Updated
- 2021/12/16
- Product number
- CS-0026810
- Product name
- MKC8866
- Purity
- 99.87%
- Packaging
- 10mg
- Price
- $850
- Updated
- 2021/12/16
MKC8866 Chemical Properties,Usage,Production
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
MKC8866 Preparation Products And Raw materials
Raw materials
Preparation Products
MKC8866 Suppliers
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