ligand
A1V2PF1
品質等級
形狀
crystals
反應適用性
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
官能基
amine
儲存溫度
2-8°C
SMILES 字串
C[C@H](NCCCCCCCCCCN)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
應用
Protein degrader building block A1V2PF1-NHEt-C10-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
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
其他說明
法律資訊
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
相關產品
产品编号
说明
价格
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
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
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