α1A-AR Degrader 9c

Uses

α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research[1].

in vivo

IC 50

α1A-adrenergic receptor: 2.86 μM (DC₅₀)

References

[1] Li Z, et al. First small-molecule PROTACs for G protein-coupled receptors: inducing α1A-adrenergic receptor degradation. Acta Pharm Sin B. 2020 Sep;10(9):1669-1679. DOI:10.1016/j.apsb.2020.01.014