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Key Documents

929484

Sigma-Aldrich

FBnG-C3-PEG1-C3-NH2 hydrochloride

≥95%

同義詞:

(R)-2-acetamido-3-((2-amino-9-(4-fluorobenzyl)-6-oxo-6,9-dihydro-1H-purin-8-yl)thio)-N-(3-(3-aminopropoxy)propyl)propanamide hydrochloride

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About This Item

經驗公式(希爾表示法):
C23H31FN8O4S · xHCl
分子量::
534.61 (free base basis)
分類程式碼代碼:
12352101
NACRES:
NA.21

品質等級

化驗

≥95%

形狀

powder

官能基

amine

儲存溫度

2-8°C

SMILES 字串

O=C1NC(N)=NC2=C1N=C(SC[C@@H](C(NCCCOCCCN)=O)NC(C)=O)N2CC3=CC=C(C=C3)F.Cl

應用

Protein degrader building block FBnG-C3-PEG1-C3-NH2 hydrochloride enables the synthesis of molecules for degradation of proteins and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a p-fluorobenzylguanine (FBnG) ligand, a 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 degrader, 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 degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.


Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation



Protein Degrader Building Blocks

法律資訊

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

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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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

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