CAS NO: | 1448189-80-7 |
规格: | 98% |
分子量: | 467.02 |
包装 | 价格(元) |
100mg | 电议 |
500mg | 电议 |
1g | 电议 |
2g | 电议 |
Background:
Protein degrader 1 hydrochloride is used in the synthesis of HaloPROTACs.
Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes.Protein degraders have the power to abrogate all of the functions of a drug target at once, including scaffolding functions which are difficult to target with small molecule inhibitors. A novel class of PROTACs that incorporate small molecule VHL ligands to successfully degrade HaloTag7 fusion proteins is developed. HaloPROTACs will inspire the development of future PROTACs with more drug-like properties. In HEK 293 cellsstably expressing GFP-HaloTag7,24 hour treatment with HaloPROTAC1 leads to less than 20% degradation, the longer HaloPROTAC2 leads to nearly 70% degradation of GFP-Halotag7 at 2.5 uM.HaloPROTACs containing protein degrader 1 leads to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used[1].
参考文献:
[1]. Buckley DL, et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins.ACS Chem Biol. 2015 Aug 21;10(8):1831-7.