产品说明
应用
Protein degrader building block A1V1PF2-OEt-C6-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:
917710 A1V1PF2-OEt
917427 A1V1PF2-OEt-C6-NH2 hydrochloride
917672 A1V1PF2-OEt-C10-NH2 hydrochloride
917923 A1V1PF2-OEt-PEG1-NH2 hydrochloride
916676 A1V1PF2-OEt-PEG3-NH2 hydrochloride
Technology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands
其他说明
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
法律信息
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
基本信息
| 经验(实验)分子式 | C31H50FN5O5 · xHCl |
| 分子量 | 591.76 (free base basis) |
产品性质
| 形式 | powder |
| 质量水平 | 100 |
| 储存温度 | 2-8℃ |
| SMILES string | C[C@H](NCCCCCCN)C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(OCC)=O)CC2=CC=C(C=C2)F)=O)=O)C(C)(C)C)=O.Cl C[C@H](NCCCCCCN)C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(OCC)=O)CC2=CC=C(C=C2)F)=O)=O)C(C)(C)C)=O.Cl |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
