sustainability
Greener Alternative Product
greener alternative category
storage temp.
2-8°C
Application
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.
Features and Benefits
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.
General description
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.
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Other Notes
QuicTPD Acid Screening Set
PROTAC Coupling Model Calculations available under the More Documents section below.
PROTAC Coupling Model Calculations available under the More Documents section below.
Legal Information
QuicTPD is a trademark of Merck KGaA, Darmstadt, Germany
signalword
Danger
Hazard Classifications
Acute Tox. 3 Oral - Acute Tox. 4 Dermal - Eye Irrit. 2 - Repr. 1A - Skin Irrit. 2 - STOT RE 2 - STOT SE 3
target_organs
Blood, Respiratory system
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation
Charles et al.
ACS Medicinal Chemistry Letters, 13(7), 1182-1190 (2022)
Accelerating PROTACs Discovery Through a Direct-to-Biology Platform Enabled by Modular Photoclick Chemistry
Ke-Nian et, al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany) (2024)
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
商品
Discover QuicTPD™ Acid/Amine Screening Sets for rapid, high-throughput PROTAC® synthesis, streamlining targeted protein degradation research.
相关内容
Join our webinar to explore the role of the orphan citron rho-interacting kinase (CITK) in cell division and its potential as a target for cancer therapies using proteolysis targeting chimeras (PROTACs).
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