产品说明
应用
Protein degrader building block Thalidomide-Photoswitch3-NH2 hydrochloride enables the synthesis of PHOtochemically TArgeting Chimeras (PHOTACs), or photoswitchable proteolysis-targeting chimeras (PROTACs) that can be reversibly activated with different wavelengths of light. Developed in the Trauner and Pagano labs, PHOTACs are inactive in the dark but are activated to the cis isomer via irradiation at 390 nm and reversibly deactivated at wavelengths above 450 nm. As described in Reynders et al, this conjugate was used to prepare PHOTAC-I-10 and PHOTAC-II-6 and contains a Cereblon (CRBN)-recruiting ligand, an azobenzene photoswitchable crosslinker, and pendant amine for reactivity with an acid on the target warhead. Light-mediated control of the resulting PHOTAC affords advanced temporal and spatial control of targeted protein degradation.
Suggested wavelengths for photoswitching:
- Switch to cis isomer: 390 nm (380-400 nm)
- Switch to trans isomer (thermally more stable isomer): >450 nm
Browse our full offering of degrader building blocks that streamlines the synthesis of degrader libraries.
Learn more:
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Portal: Building PROTAC Degraders for Targeted Protein Degradation
其他说明
PHOTACs enable optical control of protein degradation
PhotoPROTACs: A Novel Biotechnology for Cancer Treatment
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 | C27H22N6O6 · xHCl |
| 分子量 | 526.50 (free base basis) |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% |
| 形式 | solid |
| 储存温度 | 2-8℃ |
| SMILES string | O=C1N(C2C(NC(CC2)=O)=O)C(C3=C1C=CC=C3OCC(NC4=CC=C(/N=N/C5=CC=C(N)C=C5)C=C4)=O)=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 |
