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Key Documents

917710

Sigma-Aldrich

A1V1PF2-OEt

≥95%

Synonyme(s) :

AVP ligand, Ethyl (S)-2-((S)-1-((S)-2-((S)-2-aminopropanamido)-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamido)-3-(4-fluorophenyl)propanoate, IAP E3 ligase lead for protein degrader research, SNIPER building block

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About This Item

Formule empirique (notation de Hill):
C25H37FN4O5
Poids moléculaire :
492.58
Code UNSPSC :
41116105
Nomenclature NACRES :
NA.22

ligand

A1V1PF2

Niveau de qualité

Pureté

≥95%

Forme

powder

Pertinence de la réaction

reagent type: ligand

Groupe fonctionnel

amine

Température de stockage

2-8°C

Chaîne SMILES 

N[C@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(OCC)=O)CC2=CC=C(C=C2)F)=O)=O)C(C)(C)C)=O)C

Application

A1V1PF2-OEt is an in silico-derived inhibitor of apoptosis protein (IAP)-recruiting ligand for targeted protein degradation and SNIPER (specific and non-genetic IAP-dependent protein erasers) development, launched in partnership with ComInnex. Learn more about the novel IAP ligands generated through virtual screening of AVP mimetics in our Technology Spotlight. An N-terminal variant of A1V1PF2-OEt is also available as BocA1V1PF2 (917478).

A1V1PF2-OEt conjugates are also available for degrader synthesis. Browse our full synthesis offering here: Browse our full synthesis offering here for streamlining SNIPER and PROTAC® degrader libraries: Degrader Building Blocks

917427 A1V1PF2-OEt-C6-NH2 hydrochloride
917672 A1V1PF2-OEt-C10-NH2 hydrochloride
917923 A1V1PF2-OEt-PEG1-NH2 hydrochloride
916676 A1V1PF2-OEt-PEG3-NH2 hydrochloride

Technology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands

Informations légales

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

Produit(s) apparenté(s)

Réf. du produit
Description
Tarif

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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Consulter la Bibliothèque de documents

Mikihiko Naito et al.
Drug discovery today. Technologies, 31, 35-42 (2019-06-16)
The induction of protein degradation by chimeric small molecules represented by proteolysis-targeting chimeras (PROTACs) is an emerging approach for novel drug development. We have developed a series of chimeric molecules termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein
Nobumichi Ohoka et al.
The Journal of biological chemistry, 292(11), 4556-4570 (2017-02-06)
Many diseases, especially cancers, result from aberrant or overexpression of pathogenic proteins. Specific inhibitors against these proteins have shown remarkable therapeutic effects, but these are limited mainly to enzymes. An alternative approach that may have utility in drug development relies
Tasuku Ishida et al.
SLAS discovery : advancing life sciences R & D, 26(4), 484-502 (2020-11-05)
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are a new modality of chemical tools and potential therapeutics to understand and treat human disease. A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to

Articles

Targeted protein degradation reduces disease-relevant proteins in cells using small molecules, hijacking endogenous proteolysis systems.

Targeted protein degradation reduces disease-relevant proteins in cells using small molecules, hijacking endogenous proteolysis systems.

Targeted protein degradation reduces disease-relevant proteins in cells using small molecules, hijacking endogenous proteolysis systems.

Targeted protein degradation reduces disease-relevant proteins in cells using small molecules, hijacking endogenous proteolysis systems.

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