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917222

Sigma-Aldrich

A1V2PF1-NHEt

≥95%

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Synonym(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
Empirical Formula (Hill Notation):
C27H41N5O4
Molecular Weight:
499.65
UNSPSC Code:
41116105
NACRES:
NA.22

ligand

A1V2PF1

Quality Level

assay

≥95%

form

powder

reaction suitability

reagent type: ligand

functional group

amine

storage temp.

2-8°C

SMILES string

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

Application

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

Legal Information

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

related product

Product No.
Description
Pricing

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_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

Articles

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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