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920843

Sigma-Aldrich

(S,R,S)-VL285 Phenol-PEG1-piperazine hydrochloride

同義詞:

(2S,4R)-4-Hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)-2-{2-[2-(piperazin-1-yl)ethoxy]ethoxy}phenyl]methyl}-1-[(2S)-3-methyl-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)butanoyl]pyrrolidine-2-carboxamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, VHL protein degrader building block for PROTAC® research

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About This Item

經驗公式（希爾表示法）:
C37H48N6O6S · xHCl
分子量：:
704.88 (free base basis)
MDL號碼:
MFCD34549909
分類程式碼代碼:
51453014
NACRES:
NA.22

ligand

VL285 phenol

品質等級

100

形狀

solid

反應適用性

reagent type: ligand-linker conjugate

儲存溫度

2-8°C

SMILES 字串

O=C([C@@H]1C[C@@H](O)CN1C([C@H](C(C)C)N2CC(C=CC=C3)=C3C2=O)=O)NCC4=CC=C(C5=C(C)N=CS5)C=C4OCCOCCN6CCNCC6.Cl

InChI 密鑰

KONSJOIGQYDABI-FQHRNBDGSA-N

相關類別

應用

Protein degrader building block (S,R,S)-VL285 Phenol-PEG1-piperazine hydrochloride 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 with alternative exit vector from the widely used VH032 (901490), a semi-flexible PEG linker, and a pendant amine for reactivity with a carboxylic acid 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 terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

其他說明

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

法律資訊

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

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儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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分析證明 (COA)

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Blake E Smith et al.
Nature communications, 10(1), 131-131 (2019-01-12)
PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted degradation. Many potent PROTACs with specificity for dissimilar targets have been developed; however, the factors governing degradation selectivity within
Dennis L Buckley et al.
ACS chemical biology, 10(8), 1831-1837 (2015-06-13)
Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use of PROTACs, heterobifunctional molecules that can recruit specific E3 ligases to a desired protein of interest.
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
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

文章

針對蛋白質降解的降解器構件

Protein Degrader Building Blocks 是一系列交聯劑-E3 配體結合物，具有懸垂功能基團，可與目標配體共價連結。

Degrader Building Blocks for Targeted Protein Degradation

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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