HaloPROTAC 3

HaloTag is a self-labeling protein tag engineered from the haloalkane dehalogenase DhaA, originally isolated from Rhodococcus rhodochrous. Its active site binds chloroalkane (CA)substrates, forming an irreversible covalent bond. This stable linkage between the HaloTag protein and its ligand enables rapid and efficient isolation and purification of tagged proteins. HaloPROTAC3 is a class of PROTACs (Proteolysis Targeting Chimeras) that incorporate small molecule VHL (Von Hippel-Lindau) ligands to effectively degrade HaloTag7 fusion proteins. This compound is a highly potent and efficacious degrader, demonstrating a DC50 of 19 nM against GFP-HaloTag7 fusion proteins. Furthermore, HaloPROTAC3 achieves up to 90% degradation of GFP-HaloTag7 at a concentration of 625 nM. It binds to the VHL E3 ligase with an IC50 of 0.54 ?M, highlighting its strong affinity and potential as a precision tool in targeted protein degradation studies.

References

Buckley, D. L., Raina, K., Darricarrere, N., Hines, J., Gustafson, J. L., Smith, I. E., Miah, A. H., Harling, J. D., & Crews, C. M. (2015). HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. ACS Chemical Biology, 10(8), 1831–1837. https://doi.org/10.1021/acschembio.5b00442

Documents 

Datasheet          MSDS

Citations

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