相关类别
一般描述
QTPD Amine 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 amine terminal.
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应用
This set can be used for reacting with warheads/ligands for targets of interest with solvent exposed pendant carboxylic acid 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 Amine Screening Set
PROTAC Coupling Model Calculations available under the More Documents section below.
PROTAC Coupling Model Calculations available under the More Documents section below.
法律信息
QuicTPD is a trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Danger
危险声明
危险分类
Repr. 1B - STOT RE 2
靶器官
Blood
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
Accelerating PROTACs Discovery Through a Direct-to-Biology Platform Enabled by Modular Photoclick Chemistry
Yan KN, et.al
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 11 (2024)
Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation
Hendrick CE, et.al
ACS Medicinal Chemistry Letters, 13, 1182-1190 (2022)
Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery
Wang Z, et.al
Nature Communications, 14, 8437-8437 (2023)
Integrated Direct-to-Biology Platform for the Nanoscale Synthesis and Biological Evaluation of PROTACs
Stevens R, et.al
Journal of Medicinal Chemistry, 66, 15437-15452 (2023)
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
商品
Discover QuicTPD™ Acid/Amine Screening Sets for rapid, high-throughput PROTAC® synthesis, streamlining targeted protein degradation research.
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