For research use only. Not for therapeutic Use.
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 (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity[1][2].
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].
| Catalog Number | I045573 |
| CAS Number | 1033781-20-2 |
| Synonyms | (2R)-3-[3-[(E)-N-[(4-bromophenyl)methoxy]-C-methylcarbonimidoyl]phenyl]-2-ethoxypropanoic acid |
| Molecular Formula | C20H22BrNO4 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H22BrNO4/c1-3-25-19(20(23)24)12-16-5-4-6-17(11-16)14(2)22-26-13-15-7-9-18(21)10-8-15/h4-11,19H,3,12-13H2,1-2H3,(H,23,24)/b22-14+/t19-/m1/s1 |
| InChIKey | GWSVRVKPZVYTCS-VZMFNRANSA-N |
| SMILES | CCOC(CC1=CC(=CC=C1)C(=NOCC2=CC=C(C=C2)Br)C)C(=O)O |
| Reference | [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. |
