《Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5-a]pyrimidine-Based Inhibitors Targeting the DCN1-UBC12 Protein-Protein Interaction》 was written by Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Yang, Linlin; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, MAA; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Wang, Shaomeng; Liu, Hong-Min. Application of 4949-44-4This research focused ontriazolo pyrimidine derivative preparation DCN1 UBC12 protein interaction cancer. The article conveys some information:
The cullin-RING ubiquitin ligases (CRLs) are responsible for about 20% of cellular protein degradation and regulate diverse cellular processes, and the dysfunction of CRLs is implicated in human diseases. Targeting the CRLs has become an emerging strategy for the treatment of human diseases. Herein, we describe the discovery of a hit compound from our inhouse library and further structure-based optimizations, which have enabled the identification of new triazolo[1,5-a]pyrimidine-based inhibitors targeting the DCN1-UBC12 interaction. Compound WS-383 blocks the DCN1-UBC12 interaction (IC50 = 11 nM) reversibly and shows selectivity over selected kinases. WS-383 exhibits cellular target engagement to DCN1 in MGC-803 cells. WS-383 inhibits Cul3/1 neddylation selectively over other cullins and also induces accumulation of p21, p27, and NRF2. Collectively, targeting the DCN1-UBC12 interaction would be a viable strategy for selective neddylation inhibition of Cul3/1 and may be of therapeutic potential for disease treatment in which Cul3/1 is dysregulated. After reading the article, we found that the author used Ethyl 3-oxopentanoate(cas: 4949-44-4Application of 4949-44-4)
Ethyl 3-oxopentanoate(cas: 4949-44-4) belongs to ketone compounds. They are most widely used as solvents, especially in industries manufacturing explosives, lacquers, paints, and textiles. Ketones are also used in tanning, as preservatives, and in hydraulic fluids.Application of 4949-44-4
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