Product Details of 939983-66-1On May 9, 2013 ,《Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Vu, Binh; Wovkulich, Peter; Pizzolato, Giacomo; Lovey, Allen; Ding, Qingjie; Jiang, Nan; Liu, Jin-Jun; Zhao, Chunlin; Glenn, Kelli; Wen, Yang; Tovar, Christian; Packman, Kathryn; Vassilev, Lyubomir; Graves, Bradford. The article conveys some information:
The p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of cellular responses to stress. It is controlled by its neg. regulator MDM2, which binds directly to p53 and inhibits its transcriptional activity. MDM2 also targets p53 for degradation by the proteasome. Many tumors produce high levels of MDM2, thereby impairing p53 function. Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment. RG7112 (2g) is the first clin. small-mol. MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts. In the experimental materials used by the author, we found 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1Product Details of 939983-66-1)
1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1) is a member of sulfones.The sulfones, like the sulfonamides, are structural analogs of para-aminobenzoic acid that interfere with folic acid metabolism by acting as competitive inhibitors of dihydropteroate synthetase. All sulfones of clinical value are derivatives of dapsone, the most widely used member of this class.Product Details of 939983-66-1
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics