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916935

A1V2PF2-NHEt-PEG₁-NH₂

Name: A1V2PF2-NHEt-PEG<SUB>1</SUB>-NH<SUB>2</SUB>
Brand: ALDRICH

Synonyme(s) :

(S)-1-((S)-2-((S)-2-((2-(2-Aminoethoxy)ethyl)amino)propanamido)-2-cyclohexylacetyl)-N-((S)-1-(ethylamino)-3-(4-fluorophenyl)-1-oxopropan-2-yl)pyrrolidine-2-carboxamide, AVP conjugate for IAP-mediated protein degrader development, SNIPER building block

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About This Item

Formule empirique (notation de Hill):

C₃₁H₄₉FN₆O₅

Poids moléculaire :

604.76

Code UNSPSC :

41116105

Nomenclature NACRES :

NA.22

ligand

A1V2PF2

Niveau de qualité

100

Forme

powder

Pertinence de la réaction

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Groupe fonctionnel

amine

Température de stockage

2-8°C

Chaîne SMILES

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

Catégories apparentées

Biologie chimique

Building blocks d'agents de dégradation des protéines

Application

Protein degrader building block A1V2PF2-NHEt-PEG₁-NH₂ 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:
916714 A1V2PF2-NHEt
917931 A1V2PF2-NHEt-C₆-NH₂
916684 A1V2PF2-NHEt-C₁₀-NH₂
916935 A1V2PF2-NHEt-PEG₁-NH₂
917192 A1V2PF2-NHEt-PEG₃-NH₂

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

Autres remarques

In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

SNIPERs−Hijacking IAP activity to induce protein degradation

E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones

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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E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones.

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

SNIPERs-Hijacking IAP activity to induce protein degradation.

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

Articles

Degrader Building Blocks with IAP In Silico-Derived Ligands

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

Accelerating Protein Degrader Discovery with IAP

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

Degrader Building Blocks for Targeted Protein Degradation

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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