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Merck
CN
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安全信息

936588

Sigma-Aldrich

(S,R,S)-AHPC-acetamido-O-PEG2-C1-acid

≥95%

别名:

(4R)-N-[2-[2-[2-(Carboxymethoxy)ethoxy]ethoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide, (S)-13-[(2S,4R)-4-Hydroxy-2-[[4-(4-methylthiazol-5-yl)benzyl]carbamoyl]pyrrolidin-1-ylcarbonyl]-14,14-dimethyl-11-oxo-3,6,9-trioxa-12-azapentadecanoic acid, (S)-13-[(2S,4R)-4-Hydroxy-2-[[4-(4-methylthiazol-5-yl)benzyl]carbamoyl]pyrrolidine-1-carbonyl]-14,14-dimethyl-11-oxo-3,6,9-trioxa-12-azapentadecanoic acid, L-Prolinamide, N-[2-[2-[2-(carboxymethoxy)ethoxy]ethoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-

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About This Item

经验公式（希尔记法）:
C30H42N4O9S
CAS号:
2172820-10-7
分子量:
634.74
MDL编号:
MFCD33020891
UNSPSC代码:
12352106
NACRES:
NA.22

ligand

VH032

质量水平

100

方案

≥95%

表单

powder or crystals

颜色

white to beige

储存温度

2-8°C

SMILES字符串

C([C@@H](NC(COCCOCCOCC(O)=O)=O)[C@](C)(C)C)(=O)N1[C@H](C(NCC2=CC=C(C=C2)C3=C(C)N=CS3)=O)C[C@@H](O)C1

InChI

1S/C30H42N4O9S/c1-19-26(44-18-32-19)21-7-5-20(6-8-21)14-31-28(39)23-13-22(35)15-34(23)29(40)27(30(2,3)4)33-24(36)16-42-11-9-41-10-12-43-17-25(37)38/h5-8,18,22-23,27,35H,9-17H2,1-4H3,(H,31,39)(H,33,36)(H,37,38)/t22-,23+,27-/m1/s1

InChI key

IVARPPZGMUAWCE-QSEAXJEQSA-N

应用

(S,R,S)-AHPC-acetamido-O-PEG2-C1-acid is a functionalized von Hippel-Lindau (VHL) ligand. It contains a terminal carboxyl group for conjugation with amine linkers. A basic building block for development of a protein degrader library.

Technology Spotlight:

Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks

其他说明

Targeted Protein Degradation by Small Molecules


Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O′PROTAC): Effective Targeting of LEF1 and ERG


Small-Molecule PROTACS: New Approaches to Protein Degradation


Targeted Protein Degradation: from Chemical Biology to Drug Discovery


Impact of linker length on the activity of PROTACs

法律信息

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000303202
0000303202
0000289942
0000289942

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Jingwei Shao et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 8(20), e2102555-e2102555 (2021-08-17)
DNA-binding proteins, including transcription factors (TFs), play essential roles in various cellular processes and pathogenesis of diseases, deeming to be potential therapeutic targets. However, these proteins are generally considered undruggable as they lack an enzymatic catalytic site or a ligand-binding
Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can

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