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Merck
모든 사진(2)

문서

917451

Sigma-Aldrich

A1V2PF1-NHEt-PEG1-NH2

≥95%

동의어(들):

(S)-1-((S)-2-((S)-2-((2-(2-Aminoethoxy)ethyl)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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About This Item

실험식(Hill 표기법):
C31H50N6O5
Molecular Weight:
586.77
UNSPSC 코드:
41116105
NACRES:
NA.22

ligand

A1V2PF1

Quality Level

분석

≥95%

형태

powder

반응 적합성

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

작용기

amine

저장 온도

2-8°C

SMILES string

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

애플리케이션

Protein degrader building block A1V2PF1-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:
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

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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

문서

This product is a plate of 80 ligands against the E3 ligase IAP The ligands were designed by ComInnex using a computational approach. Linkers can be added to these ligands allowing attachment to target ligands to create bifunctional targeted protein degraders. The ligands can also be used to discover molecular glues that bring together the IAP E3 ligase and a target.

자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

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