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917222

Sigma-Aldrich

A1V2PF1-NHEt

≥95%

Sinônimo(s):

(S)-1-((S)-2-((S)-2-Aminopropanamido)-2-cyclohexylacetyl)-N-((S)-1-(ethylamino)-1-oxo-3-phenylpropan-2-yl)pyrrolidine-2-carboxamide, AVP ligand, IAP E3 ligase lead for protein degrader research, SNIPER building block

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About This Item

Fórmula empírica (Notação de Hill):
C27H41N5O4
Peso molecular:
499.65
Código UNSPSC:
41116105
NACRES:
NA.22

ligand

A1V2PF1

Nível de qualidade

Ensaio

≥95%

forma

powder

adequação da reação

reagent type: ligand

grupo funcional

amine

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

N[C@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(NCC)=O)CC2=CC=CC=C2)=O)=O)C3CCCCC3)=O)C

Aplicação

A1V2PF1-NHEt 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 A1V2PF1-NHEt is also available as BocA1V2PF1 (916978).

A1V2PF1-NHEt conjugates are also available for degrader synthesis. Browse our full synthesis offering here for streamlining SNIPER and PROTAC® degrader libraries: Degrader Building Blocks
916943 A1V2PF1-NHEt-C6-NH2
917206 A1V2PF1-NHEt-C10-NH2
917451 A1V2PF1-NHEt-PEG1-NH2
917702 A1V2PF1-NHEt-PEG3-NH2

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

Informações legais

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

produto relacionado

Nº do produto
Descrição
Preços

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°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

Artigos

Targeted protein degradation (TPD) is an emerging strategy that uses small molecules to hijack endogenous proteolysis systems to degrade disease-relevant proteins and thus reduce their abundance in cells.

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

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.

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