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Merck
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QCRBNSET

QuicTPD™ CRBN ligand Set

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NACRES:
NA.21

Key Documents

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packaging

pkg of 50 mg

sustainability

Greener Alternative Product

greener alternative category

DfS-Developed

storage temp.

2-8°C

Quality Level

100

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Application

Useful for construction of CRBN based partial protacs of full protacs, by utilizing the amine terminus to add suitable linkers with peptide coupling reactions. These can also be used as controls/competitors to confirm target engagement of putative protacs.

Features and Benefits

Quantities provided are sufficient to do atleast 96 reactions at 2 micromole each with a D2B approach with a library of suitable bifunctional linkers ending in carboxylic acid terminus to generate a library of partial protacs or full protacs.

General description

5-Amino Thalidomide, Lenalidomide, Pomalidomide and C-5 Lenalidomide are recruiters of CRBN protein that can be leveraged for targeted protein degradation research. They are provided at 50 mg each.
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Other Notes

CRBN Ligand Set part of QuicTPD™ kit

Legal Information

QuicTPD is a trademark of Merck KGaA, Darmstadt, Germany

pictograms

Skull and crossbonesHealth hazard
GHS06,GHS08

signalword

Danger

Hazard Classifications

Acute Tox. 3 Oral - Acute Tox. 4 Dermal - Repr. 1A - STOT RE 2

target_organs

Blood

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

Regulatory Information

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Aleša Bricelj et al.
ACS medicinal chemistry letters, 12(11), 1733-1738 (2021-11-20)
Proteolysis targeting chimeras (PROTACs) hijacking the cereblon (CRBN) E3 ubiquitin ligase have emerged as a novel paradigm in drug development. Herein we found that linker attachment points of CRBN ligands highly affect their aqueous stability and neosubstrate degradation features. This
Alexandru D Buhimschi et al.
Biochemistry, 57(26), 3564-3575 (2018-06-01)
Inhibition of Bruton's tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies, yet >80% of CLL patients develop resistance due to a cysteine
Georg E Winter et al.
Science (New York, N.Y.), 348(6241), 1376-1381 (2015-05-23)
The development of effective pharmacological inhibitors of multidomain scaffold proteins, notably transcription factors, is a particularly challenging problem. In part, this is because many small-molecule antagonists disrupt the activity of only one domain in the target protein. We devised a
Gang Lu et al.
Science (New York, N.Y.), 343(6168), 305-309 (2013-12-03)
Thalidomide-like drugs such as lenalidomide are clinically important treatments for multiple myeloma and show promise for other B cell malignancies. The biochemical mechanisms underlying their antitumor activity are unknown. Thalidomide was recently shown to bind to, and inhibit, the cereblon

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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QuicTPDTM Amine Screening Set
QuicTPDTM Acid Screening Set

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