901511
(S,R,S)-AHPC-PEG3-NH2 hydrochloride
≥95%
别名:
(2S,4R)-1-((S)-14-Amino-2-(tert-butyl)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader, VH032 conjugate
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关于此项目
经验公式（希尔记法）:
C30H45N5O7S · xHCl
化学文摘社编号:
分子量:
619.77 (free base basis)
MDL编号:
UNSPSC代码:
12352101
NACRES:
NA.22
ligand
VH032
质量水平
方案
≥95%
表单
powder or crystals
反应适用性
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
官能团
amine
储存温度
2-8°C
SMILES字符串
O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(COCCOCCOCCN)=O)=O.Cl
InChI key
ZOYHUTRHKHRRPK-QVRKWNSCSA-N
应用
Protein degrader builiding block (S,R,S)-AHPC-PEG3-NH2 (HCl salt) enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)
Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)
其他说明
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands
Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation
Targeted Protein Degradation by Small Molecules
Impact of linker length on the activity of PROTACs
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands
Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation
Targeted Protein Degradation by Small Molecules
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
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2
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
此项目有
Philipp Ottis et al.
ACS chemical biology, 12(10), 2570-2578 (2017-08-03)
Proteolysis targeting chimera (PROTAC) technology, the recruitment of E3 ubiquitin ligases to induce the degradation of a protein target, is rapidly impacting chemical biology, as well as modern drug development. Here, we explore the universality of this approach by evaluating
David Remillard et al.
Angewandte Chemie (International ed. in English), 56(21), 5738-5743 (2017-04-19)
The bromodomain-containing protein BRD9, a subunit of the human BAF (SWI/SNF) nucleosome remodeling complex, has emerged as an attractive therapeutic target in cancer. Despite the development of chemical probes targeting the BRD9 bromodomain, there is a limited understanding of BRD9
Kwok-Ho Chan et al.
Journal of medicinal chemistry, 61(2), 504-513 (2017-06-09)
The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a linker. Here we examined the impact of derivatizing two different BET bromodomain
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
商品
Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.
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