Protein degrader 1 hydrochloride

A PROTAC building block

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库存: 现货

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数量
100mg

￥550.00

440.00

- +
500mg

￥2050.00

1640.00

- +
1g

￥3287.00

2630.00

- +
2g

￥5487.00

4390.00

- +

已选 0 种 0 瓶

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货号: ajci22846
CAS: 1448189-80-7
别名: (2S,4R)-1-((S)-2-氨基-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺盐酸盐,VH032-NH2 hydrochloride; VHL ligand 1 hydrochloride
分子式: C22H31ClN4O3S
分子量: 467.02
纯度: >98%
溶解度: DMSO : 150 mg/mL (321.19 mM);Water : 50 mg/mL (107.06 mM)
储存: Store at -20°C
库存: 现货

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.