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[CAS NO. 1338934-59-0] MKC8866
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-104040 |
| Brand: | MCE |
| CAS: | 1338934-59-0 |
Overview
| MDL | MFCD31540824 |
|---|---|
| Molecular Weight | 361.35 |
| Molecular Formula | C18H19NO7 |
| SMILES | O=CC1=C(O2)C(C(C)=C(CC(N3CCOCC3)=O)C2=O)=CC(OC)=C1O |
8 Publications Citing Use of MCE
- [1]Science. 2019 Jul 19;365(6450):eaau6499.
- [2]J Exp Med. 2022 Nov 7;219(11):e20221085.
- [3]Cancer Lett. 2020 Oct 10;490:76-88.
- [4]Cell Death Dis. 2022 Apr 20;13(4):384.
- [5]Int J Mol Sci. 2022, 23(16), 9113.
- [6]J Diabetes Investig. 2023 Jan 24.
- [7]Front Pharmacol. 2022 Mar 21;13:854506.
- [8]Sci Rep. 2019 Mar 1;9(1):3210.
Summary
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC 50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC 50 of 0.52 μM and unstresses RPMI 8226 cells with an IC 50 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
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. |
Appearance
Solid
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
DMSO : 16.67 mg/mL ( 46.13 mM ; Need ultrasonic)
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 |
References
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