Tag: 323.142

Development of selective small molecule MDM2 degraders based on nutlin was written by Wang, Bo;Wu, Suzhen;Liu, Jin;Yang, Ka;Xie, Haibo;Tang, Weiping. And the article was included in European Journal of Medicinal Chemistry in 2019.Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione This article mentions the following:

Tumor suppressor protein p53 is important to the regulation of many cellular processes and the prevention of cancer development. In some cancer cells, the function of p53 is inhibited by murine double minute 2 protein (MDM2). To restore the function of p53, the inhibition or depletion of MDM2 has become a potential therapeutic treatment. We have successfully developed a series of small mol. MDM2 degraders that can promote the proteolysis of MDM2 oncoprotein, thus reactivating tumor suppressor p53. The superior degrader features a nutlin-based MDM2 ligand and a lenalidomide-based cereblon E3 ubiquitin ligase ligand with a short linker between the two ligands. At low nanomolar concentrations in RS4; 11 leukemia cells, this degrader promotes efficient degradation of MDM2. It also inhibits the proliferation of leukemia cells with an IC₅₀ value of 3.2 nM and induces apoptosis effectively. All of these data indicate that MDM2 degraders are promising therapeutics for the treatment of cancers, such as leukemia. In the experiment, the researchers used many compounds, for example, 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione (cas: 2093387-36-9Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione).

3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione (cas: 2093387-36-9) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Development of selective small molecule MDM2 degraders based on nutlin was written by Wang, Bo;Wu, Suzhen;Liu, Jin;Yang, Ka;Xie, Haibo;Tang, Weiping. And the article was included in European Journal of Medicinal Chemistry in 2019.Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione This article mentions the following:

Tumor suppressor protein p53 is important to the regulation of many cellular processes and the prevention of cancer development. In some cancer cells, the function of p53 is inhibited by murine double minute 2 protein (MDM2). To restore the function of p53, the inhibition or depletion of MDM2 has become a potential therapeutic treatment. We have successfully developed a series of small mol. MDM2 degraders that can promote the proteolysis of MDM2 oncoprotein, thus reactivating tumor suppressor p53. The superior degrader features a nutlin-based MDM2 ligand and a lenalidomide-based cereblon E3 ubiquitin ligase ligand with a short linker between the two ligands. At low nanomolar concentrations in RS4; 11 leukemia cells, this degrader promotes efficient degradation of MDM2. It also inhibits the proliferation of leukemia cells with an IC₅₀ value of 3.2 nM and induces apoptosis effectively. All of these data indicate that MDM2 degraders are promising therapeutics for the treatment of cancers, such as leukemia. In the experiment, the researchers used many compounds, for example, 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione (cas: 2093387-36-9Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione).

3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione (cas: 2093387-36-9) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Development of selective small molecule MDM2 degraders based on nutlin was written by Wang, Bo;Wu, Suzhen;Liu, Jin;Yang, Ka;Xie, Haibo;Tang, Weiping. And the article was included in European Journal of Medicinal Chemistry in 2019.Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione This article mentions the following:

Tumor suppressor protein p53 is important to the regulation of many cellular processes and the prevention of cancer development. In some cancer cells, the function of p53 is inhibited by murine double minute 2 protein (MDM2). To restore the function of p53, the inhibition or depletion of MDM2 has become a potential therapeutic treatment. We have successfully developed a series of small mol. MDM2 degraders that can promote the proteolysis of MDM2 oncoprotein, thus reactivating tumor suppressor p53. The superior degrader features a nutlin-based MDM2 ligand and a lenalidomide-based cereblon E3 ubiquitin ligase ligand with a short linker between the two ligands. At low nanomolar concentrations in RS4; 11 leukemia cells, this degrader promotes efficient degradation of MDM2. It also inhibits the proliferation of leukemia cells with an IC₅₀ value of 3.2 nM and induces apoptosis effectively. All of these data indicate that MDM2 degraders are promising therapeutics for the treatment of cancers, such as leukemia. In the experiment, the researchers used many compounds, for example, 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione (cas: 2093387-36-9Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione).

3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione (cas: 2093387-36-9) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Safety of 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem