packaging
pkg of 10 mg
sustainability
Greener Alternative Product
greener alternative category
storage temp.
2-8°C
Quality Level
Other Notes
Negative Control Set part of QuicTPD™ kit
Legal Information
QuicTPD is a trademark of Merck KGaA, Darmstadt, Germany
Application
Useful for construction of small molecules structurally similar to PROTACs of interest but with no inherent degradation action in themselves serving as negative control.
Features and Benefits
Structural similarity to active CRBN/VHL ligands is optimal for construction of negative controls. The amino terminus in each can be used for attaching bifunctional linkers with reactions such as peptide coupling.
General description
N-Methylated Pomalidomide is a ligand used as a negative control for pomalidomide in the recuitment of Cereblon (CRBN) protein, whereas (S,S,S) AHPC-hydrochloride is a ligand used as negative control for (S,R,S)-AHPC in the recruitment of von-Hippel Lindau (VHL) protein. N-methylation of pomalidomide or the inversion of stereochemistry to yield of (S,S,S) AHPC prevents binding to CRBN and VHL proteins. These are provided at 10mg each.
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存储类别
11 - Combustible Solids
wgk
WGK 3
法规信息
新产品
此项目有
Andrew P Crew et al.
Journal of medicinal chemistry, 61(2), 583-598 (2017-07-12)
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted degraders is still relatively young, the potential for this modality
Christian Steinebach et al.
ACS chemical biology, 13(9), 2771-2782 (2018-08-18)
The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide, all approved for the treatment of multiple myeloma, induce targeted ubiquitination and degradation of Ikaros (IKZF1) and Aiolos (IKZF3) via the cereblon (CRBN) E3 ubiquitin ligase. IMiD-based proteolysis-targeting chimeras (PROTACs) can efficiently
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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