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[CAS NO. 1033781-20-2] KS15
| 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-115672 |
| Brand: | MCE |
| CAS: | 1033781-20-2 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 420.30 |
| Molecular Formula | C20H22BrNO4 |
| SMILES | CCO[C@@H](C(O)=O)CC1=CC(/C(C)=N/OCC2=CC=C(C=C2)Br)=CC=C1 |
Summary
KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer . KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC 50 =4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity [1] [2] .
In Vitro
Applications of KS15 at different concentrations from 1 μM to 10 μM restored the E-box-driven luciferase activities in a dose-dependent manner, indicating that KS15 evidently impairs the suppressive actions of CRYs on CLOCK:BMAL1-induced transcription. KS15 inhibits the interactions between CRYs and BMAL1, resulting in the enhanced transcriptional activity in the core loop of the molecular circadian clock
[1]
.
KS15 directly binds to the C-terminal region of cryptochromes (CRYs: CRY1 and CRY2) and enhances E-box-mediated transcription
[2]
.
KS15 decreases the speed of cell growth and increased the chemosensitivity of MCF-7 cells to Doxorubicin and Tamoxifen. KS15 exerts an anti-proliferative effect and increases sensitivity to anti-tumor drugs in a specific type of breast cancer
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Liquid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 237.93 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3793 mL | 11.8963 mL | 23.7925 mL |
| 5 mM | 0.4759 mL | 2.3793 mL | 4.7585 mL |
| 10 mM | 0.2379 mL | 1.1896 mL | 2.3793 mL |
References
- [1] Chun SK, et al. A synthetic cryptochrome inhibitor induces anti-proliferative effects and increases chemosensitivity in human breast cancer cells. Biochem Biophys Res Commun. 2015;467(2):441-446.
- [2] Jang J, et al. The cryptochrome inhibitor KS15 enhances E-box-mediated transcription by disrupting the feedback action of a circadian transcription-repressor complex. Life Sci. 2018;200:49-55.
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