产品描述
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.
体外活性
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].
Cas No.
1033781-20-2
分子式
C20H22BrNO4
分子量
420.3
别名
KS15
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years