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916951

Sigma-Aldrich

BocA1V2PF1-NHPEG1-NH2

Synonyme(s) :

AVP conjugate for IAP-mediated protein degrader development, SNIPER building block

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About This Item

Formule empirique (notation de Hill):
C34H54N6O7
Poids moléculaire :
658.83
Code UNSPSC :
41116105
Nomenclature NACRES :
NA.22

ligand

BocA1V2PF1

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

Catégories apparentées

Application

Protein degrader building block BocA1V2PF1-NHPEG1-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:
916978 BocA1V2PF1
917966 BocA1V2PF1-NHC6-NH2
916706 BocA1V2PF1-NHC10-NH2
916951 BocA1V2PF1-NHPEG1-NH2
917214 BocA1V2PF1-NHPEG3-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

917931

A1V2PF2-NHEt-C6-NH2

916684

A1V2PF2-NHEt-C10-NH2, ≥95%

917680

BocA1V1PF2-OPEG3-NH2 hydrochloride

917966

BocA1V2PF1-NHC6-NH2

917702

A1V2PF1-NHEt-PEG3-NH2

917451

A1V2PF1-NHEt-PEG1-NH2, ≥95%

917974

BocA1V2PF2

917710

A1V1PF2-OEt, ≥95%

917478

BocA1V1PF2, ≥95%

917214

BocA1V2PF1-NHPEG3-NH2, ≥85%

916951

BocA1V2PF1-NHPEG1-NH2

916927

BocA1V1PF2-OC6-NH2 hydrochloride, ≥95%

916676

A1V1PF2-OEt-PEG3-NH2 hydrochloride

917923

A1V1PF2-OEt-PEG1-NH2 hydrochloride

917672

A1V1PF2-OEt-C10-NH2 hydrochloride

917206

A1V2PF1-NHEt-C10-NH2

917184

BocA1V1PF2-OC10-NH2 hydrochloride

916943

A1V2PF1-NHEt-C6-NH2

916692

BocA1V2PF2-NHPEG3-NH2, ≥95%

917427

A1V1PF2-OEt-C6-NH2 hydrochloride

916706

BocA1V2PF1-NHC10-NH2

917435

BocA1V1PF2-OPEG1-NH2 hydrochloride, ≥95%

916978

BocA1V2PF1, ≥95%

917699

BocA1V2PF2-NHC10-NH2, ≥85%

917222

A1V2PF1-NHEt, ≥95%

917958

BocA1V2PF2-NHPEG1-NH2

916714

A1V2PF2-NHEt, ≥95%

917192

A1V2PF2-NHEt-PEG3-NH2, ≥95%

916935

A1V2PF2-NHEt-PEG1-NH2

917443

BocA1V2PF2-NHC6-NH2

919446

CCW16-PEG1-BocNH

CIX001

ComInnex IAP Ligand Library

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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Certificats d'analyse (COA)

Lot/Batch Number

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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

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.

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.

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.

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.

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