一般描述
(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.
应用
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.
特点和优势
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.
其他说明
VHL Ligand Set part of QuicTPD™ kit
法律信息
QuicTPD is a trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
法规信息
新产品
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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