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KS15

Catalog No. T38433 CAS 1033781-20-2

KS15 is a chemical compound that acts as an inhibitor on the interactions between cryptochromes, specifically CRY1 and CRY2, and the CLOCK: BMAL1 heterodimer. This compound, with an EC50 value of 4.9 μM, hinders the feedback actions of CRYs on E-box-dependent transcription. The CLOCK: BMAL1 heterodimer is a vital transcriptional regulator for the mammalian circadian clock. In addition, KS15 exhibits significant anti-proliferative activity.

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KS15, CAS 1033781-20-2

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Description

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].

Molecular Weight	420.303
Formula	C20H22BrNO4
CAS No.	1033781-20-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

KS15 1033781-20-2 KS-15 KS 15 inhibitor inhibit

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