Recommanded Product: 50816-19-8. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 8-Bromooctan-1-ol, is researched, Molecular C8H17BrO, CAS is 50816-19-8, about Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders. Author is Iida, Tetsuya; Itoh, Yukihiro; Takahashi, Yukari; Yamashita, Yasunobu; Kurohara, Takashi; Miyake, Yuka; Oba, Makoto; Suzuki, Takayoshi.
Lysine demethylase 5 C (KDM5C) controls epigenetic gene expression and is attracting great interest in the field of chem. epigenetics. KDM5C has emerged as a therapeutic target for anti-prostate cancer agents, and recently we identified triazole 1 as an inhibitor of KDM5C. Compound 1 exhibited highly potent KDM5C-inhibitory activity in in vitro enzyme assays, but did not show strong anticancer effects. Therefore, a different approach is needed for the development of anticancer agents targeting KDM5C. Here, we attempted to identify KDM5C degraders by focusing on a protein-knockdown strategy. Compound 3 b, which was designed based on compound 1, degraded KDM5C and inhibited the growth of prostate cancer PC-3 cells more strongly than compound 1. These findings suggest that KDM5C degraders are more effective as anticancer agents than compounds that only inhibit the catalytic activity of KDM5C.
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