储存温度
2-8°C
质量水平
一般描述
QTPD Acid set comprised of 36 partial protacs plated in duplicate with rich linker diversity, architecture and length targeting Cereblon(CRBN) and von Hippel Lindau( VHL) E3 ligases ending in a carboxylic acid terminal.
应用
This set can be used for reacting with warheads/ligands for targets of interest with solvent exposed pendant amine handles via peptide coupling reactions. Two distinct warheads can be reacted with this set to generate 72 distinct small molecule degraders that can be used for subsequent screening.
特点和优势
Representative set of partial protacs targeting both CRBN and VHL with typical PEG, hydrophobic and rigid linkers that can be used for construction of PROTACs. Customers can make screen upto 24 reaction conditions with this set and empty glass shell vials provided with the pre-plated set. Glass shell vials allow for exploration of reaction conditions tolerant to different, reagents, solvents and temperature. Miniaturized synthesis allows for reduction in solvent, reagent, water and energy usage making this a sustainable and faster route to PROTAC discovery.
其他说明
QuicTPD Acid Screening Set
储存分类代码
11 - Combustible Solids
法规信息
新产品
Charles E Hendrick et al.
ACS medicinal chemistry letters, 13(7), 1182-1190 (2022-07-22)
A platform to accelerate optimization of proteolysis targeting chimeras (PROTACs) has been developed using a direct-to-biology (D2B) approach with a focus on linker effects. A large number of linker analogs-with varying length, polarity, and rigidity-were rapidly prepared and characterized in
Ke-Nian Yan et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 11(26), e2400594-e2400594 (2024-05-01)
Proteolysis targeting chimeras (PROTACs) have emerged as a promising strategy for drug discovery and exploring protein functions, offering a revolutionary therapeutic modality. Currently, the predominant approach to PROTACs discovery mainly relies on an empirical design-synthesis-evaluation process involving numerous cycles of
Rebecca Stevens et al.
Journal of medicinal chemistry, 66(22), 15437-15452 (2023-11-07)
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules that co-opt the cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A challenge associated with PROTACs is the time and resource-intensive optimization; thus, the development of high-throughput platforms for their synthesis and
Zefeng Wang et al.
Nature communications, 14(1), 8437-8437 (2023-12-20)
Thalidomide and its analogs are molecular glues (MGs) that lead to targeted ubiquitination and degradation of key cancer proteins via the cereblon (CRBN) E3 ligase. Here, we develop a direct-to-biology (D2B) approach for accelerated discovery of MGs. In this platform
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