24522-69-8Relevant academic research and scientific papers
Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: Significance of the para-hydroxyl orientation
Baskin, Rebekah,Gali, Meghanath,Park, Sung O.,Zhao, Zhizhuang Joe,Keser, Gy?rgy M.,Bisht, Kirpal S.,Sayeski, Peter P.
, p. 1402 - 1407 (2012/04/04)
In this study, we analyzed the structure-activity relationship properties of the small molecule Jak2 inhibitor G6. We synthesized a set of derivatives containing the native para-hydroxyl structure or an alternative meta-hydroxyl structure and examined their Jak2 inhibitory properties. We found that the para-hydroxyl derivative known as NB15 had excellent Jak2 inhibitory properties in silico, in vitro, and ex vivo when compared with meta-hydroxyl derivatives. These results indicate that NB15 is a potent derivative of the Jak2 inhibitor G6, and that maintaining the para-hydroxyl orientation of G6 is critical for its Jak2 inhibitory potential.
