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916943

A1V2PF1-NHEt-C₆-NH₂

Name: A1V2PF1-NHEt-C<SUB>6</SUB>-NH<SUB>2</SUB>
Brand: ALDRICH

Szinonimák:

(S)-1-((S)-2-((S)-2-((6-Aminohexyl)amino)propanamido)-2-cyclohexylacetyl)-N-((S)-1-(ethylamino)-1-oxo-3-phenylpropan-2-yl)pyrrolidine-2-carboxamide, AVP conjugate for IAP-mediated protein degrader development, SNIPER building block

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Összes fotó(2)

About This Item

Tapasztalati képlet (Hill-képlet):

C₃₃H₅₄N₆O₄

Molekulatömeg:

598.82

UNSPSC kód:

41116105

NACRES:

NA.22

ligand

A1V2PF1

Minőségi szint

100

form

powder

reakcióalkalmasság

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

funkcionális csoport

amine

tárolási hőmérséklet

2-8°C

SMILES string

C[C@H](NCCCCCCN)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

Related Categories

Chemical Biology

Protein Degrader Building Blocks

Alkalmazás

Protein degrader building block A1V2PF1-NHEt-C₆-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:
917222 A1V2PF1-NHEt
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

Egyéb megjegyzések

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

Jogi információk

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

kapcsolódó termék

Product No.

Leírás

Árazás

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable

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Analitikai tanúsítványok (COA)

Lot/Batch Number

Sajnos jelenleg COA nem áll rendelkezésre ehhez a termékhez online.

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Dokumentumtár megtekintése

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

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

Cikkek

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.

Tudóscsoportunk valamennyi kutatási területen rendelkezik tapasztalattal, beleértve az élettudományt, az anyagtudományt, a kémiai szintézist, a kromatográfiát, az analitikát és még sok más területet.

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