Protein degrader 1 TFA (Synonyms: VH032-NH2 TFA; VHL ligand 1 TFA) |
| Katalog-Nr.GC32433 |
(S,R,S)-AHPC (VH032-NH2) TFA ist der VH032-basierte VHL-Ligand, der bei der Rekrutierung des von Hippel-Lindau (VHL)-Proteins verwendet wird. Proteinabbauer 1 TFA kann mit dem Liganden fÜr Protein (z. B. BCR-ABL1) durch einen Linker verbunden werden, um PROTACs (z. B. GMB-475) zu bilden. GMB-475 induziert den Abbau von BCR-ABL1 mit einem IC50 von 1,11 μM in Ba/F3-Zellen.
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Cas No.: 1631137-51-3
Sample solution is provided at 25 µL, 10mM.
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Protein degrader 1 TFA is a small molecule ligand for VHL, an E3 ligase which has been targeted in numerous PROTACs.
Synthesis of HaloPROTACs contains Protein degrader 1 (Degradation Inducing Moiety A). Protein degrader 1 (Degradation Inducing Moiety A) is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. HaloPROTACs containing Protein degrader 1 (Degradation Inducing Moiety A) lead to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used[1].
[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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