Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor was written by Lefranc, Julien;Schulze, Volker Klaus;Hillig, Roman Christian;Briem, Hans;Prinz, Florian;Mengel, Anne;Heinrich, Tobias;Balint, Jozsef;Rengachari, Srinivasan;Irlbacher, Horst;Stoeckigt, Detlef;Boemer, Ulf;Bader, Benjamin;Gradl, Stefan Nikolaus;Nising, Carl Friedrich;von Nussbaum, Franz;Mumberg, Dominik;Panne, Daniel;Wengner, Antje Margret. And the article was included in Journal of Medicinal Chemistry in 2020.Reference of 21867-64-1 This article mentions the following:
The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homolog IKKε are noncanonical members of the inhibitor of the nuclear factor κB (IκB) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKKε inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Reference of 21867-64-1).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Reference of 21867-64-1
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics