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916676

Sigma-Aldrich

A1V1PF2-OEt-PEG3-NH2 hydrochloride

Sinonimo/i:

AVP conjugate for IAP-mediated protein degrader development, Ethyl (S)-2-((S)-1-((2S,5S)-17-amino-2-(tert-butyl)-5-methyl-4-oxo-9,12,15-trioxa-3,6-diazaheptadecanoyl)pyrrolidine-2-carboxamido)-3-(4-fluorophenyl)propanoate hydrochloride, SNIPER building block

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About This Item

Formula empirica (notazione di Hill):
C33H54FN5O8 · xHCl
Peso molecolare:
667.81 (free base basis)
Codice UNSPSC:
41116105
NACRES:
NA.22

ligand

A1V1PF2

Livello qualitativo

Forma fisica

powder

Impiego in reazioni chimiche

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Gruppo funzionale

amine

Temperatura di conservazione

2-8°C

Stringa SMILE

C[C@H](NCCOCCOCCOCCN)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.Cl

Applicazioni

Protein degrader building block A1V1PF2-OEt-PEG3-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and SNIPER (specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers) technology. Developed in partnership with ComInnex, this conjugate contains an in silico-derived IAP-recruiting ligand, an alkyl-chain crosslinker, and a pendant amine for reactivity with an acid on a target warhead. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and protein degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, including CRBN and VHL targeted, parallel synthesis can be used to more quickly generate SNIPER and PROTAC® degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand. Learn more about the novel IAP ligands generated through virtual screening of AVP mimetics in our Technology Spotlight.Building blocks in this series:917710 A1V1PF2-OEt917427 A1V1PF2-OEt-C6-NH2 hydrochloride917672 A1V1PF2-OEt-C10-NH2 hydrochloride 917923 A1V1PF2-OEt-PEG1-NH2 hydrochloride916676 A1V1PF2-OEt-PEG3-NH2 hydrochlorideTechnology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands

Note legali

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

Prodotti correlati

N° Catalogo
Descrizione
Determinazione del prezzo

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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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

Articoli

Plate of 80 ligands against E3 ligase IAP designed by ComInnex; allows creation of bifunctional targeted protein degraders or molecular glues.

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Il team dei nostri ricercatori vanta grande esperienza in tutte le aree della ricerca quali Life Science, scienza dei materiali, sintesi chimica, cromatografia, discipline analitiche, ecc..

Contatta l'Assistenza Tecnica.