常用名:(S,R,S)-AHPC hydrochloride
产品描述:
(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).
体外活性 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 μM.HaloPROTACs containing protein degrader 1 leads to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used
别名 VHL Ligand 1 hydrochloride, ULM-1, Protein degrader 1 hydrochloride
分子量 467.03
分子式 C22H31ClN4O3S
CAS No. 1448189-80-7
存储
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度
DMSO: 10 mM
PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来,从而“劫持”细胞的泛素-蛋白酶体系统(UPS)来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标(而不是抑制靶蛋白的酶活性),目前有许多努力将先前无效的抑制剂分子改造为 PROTACs,用作下一代药物。
产地:西安
用途:科研!
厂家:西安齐岳生物科技有限公司
温馨提示:仅用于科研,不能用于人体实验!
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