Synonyms: tert-Butyl ((S)-1-(((S)-2-((S)-2-(((S)-1-((6-aminohexyl)amino)-3-(4-fluorophenyl)-1-oxopropan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-cyclohexyl-2-oxoethyl)amino)-1-oxopropan-2-yl)carbamate; AVP conjugate for IAP-mediated protein degrader development; SNIPER building block
Molecular Formula: C36H57FN6O6
Molecular Weight: 688.87
Linear Structural Formula: C36H57FN6O6
Storage: 2-8C
Application: Protein degrader building block BocA1V2PF2-NHC6-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(R) 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 BocA1V2PF2917443 BocA1V2PF2-NHC6-NH2917958 BocA1V2PF2-NHC10-NH2917958 BocA1V2PF2-NHPEG1-NH2916692 BocA1V2PF2-NHPEG3-NH2Technology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands
Legal Information: PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
Other Notes: 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 degradationE3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones