QVHLSET
QuicTPD™ VHL ligand set
General description
(S,R,S)-AHPC and (S,R,S)-AHPC-Me are recruiters of von-Hippel-Lindau (VHL) protein that can be leveraged for targeted protein degradation research. They are provided at 50 mg each.
Application
Useful for construction of VHL 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 1 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.
Other Notes
VHL Ligand Set part of QuicTPD™ kit
Legal Information
QuicTPD is a trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Regulatory Information
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Xin Han et al.
Journal of medicinal chemistry, 62(2), 941-964 (2019-01-11)
We report herein the discovery of highly potent PROTAC degraders of androgen receptor (AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent manner. ARD-69 achieves
Ashton C Lai et al.
Angewandte Chemie (International ed. in English), 55(2), 807-810 (2015-11-26)
Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging alternative therapeutic strategy with the potential to address many of the challenges currently faced in modern drug development programs. PROTAC technology employs small molecules that recruit target proteins for ubiquitination and
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