Protein degrader 1 hydrochloride |
カタログ番号GC19302 |
(S,R,S)-AHPC (VH032-NH2) 塩酸塩は、von Hippel-Lindau (VHL) タンパク質の動員に使用される VH032 ベースの VHL リガンドです。タンパク質分解剤 1 塩酸塩は、PROTAC (例えば、GMB-475) を形成するリンカーによって、タンパク質のリガンド (例えば、BCR-ABL1) に接続することができます。 GMB-475 は Ba/F3 細胞で 1.11 μM の IC50 で BCR-ABL1 の分解を誘導します。
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Cas No.: 1448189-80-7
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
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