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QAMINESET

QuicTPD™ Amine Optimization Set

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NACRES:
NA.21

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sustainability

Greener Alternative Product

greener alternative category

DfS-Developed

storage temp.

2-8°C

Quality Level

100

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Features and Benefits

Two of these PROTACs are tailored to target the CRBN E3 ligase, while the other two are directed towards VHL, incorporating both hydrophobic and hydrophilic linkers. By utilizing this optimization set, customers can explore a variety of reaction conditions—up to 24 or more—before proceeding to the complete screening set. This exploration includes testing different coupling reagents, solvents, and bases, allowing for a comprehensive assessment of the synthesis parameters that influence the efficiency and yield of the desired products.

General description

This set includes 4 representative partial PROTACs, each provided at 5 micromole quantity.
We are committed to bringing you Greener Alternative Products. This product is a Design for Sustainability (DfS) developed product, which belongs to one of the four categories of greener alternatives. Click here to view its DfS scorecard.

Other Notes

QuicTPD Amine Screening Set

Legal Information

QuicTPD is a trademark of Merck KGaA, Darmstadt, Germany

Application

The QuicTPD Amine Optimization set is designed to facilitate high throughput synthesis optimization for researchers working with PROTACs.

pictograms

Health hazardExclamation mark
GHS08,GHS07

signalword

Warning

target_organs

Blood

Storage Class

11 - Combustible Solids

wgk

WGK 3

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2 - Repr. 2 - Skin Irrit. 2 - STOT RE 2

Regulatory Information

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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
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
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

Articles

PROTAC Synthesis Kits for Targeted Protein Degradation

Discover QuicTPD™ Acid/Amine Screening Sets for rapid, high-throughput PROTAC® synthesis, streamlining targeted protein degradation research.

Related Content

Developing a CITK protein degrader

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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