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929484

FBnG-C3-PEG1-C3-NH2 hydrochloride

≥95%

Synonym(s):

(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

Empirical Formula (Hill Notation):
C23H31FN8O4S · xHCl
Molecular Weight:
534.61 (free base basis)
UNSPSC Code:
12352101
NACRES:
NA.21
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Quality Level

100

assay

≥95%

form

powder

functional group

amine

storage temp.

2-8°C

SMILES string

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

Application

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

Other Notes

Targeted Protein Degradation by Small Molecules

AUTACs: Cargo-Specific Degraders Using Selective Autophagy

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_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