AR antagonist 1 

AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

IC50: androgen receptor^[1]

AR antagonist 1 (compound 29) is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader.
AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders.
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein.
PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

278.78

C₁₅H₁₉ClN₂O

1818885-54-9

N#CC1=CC=C(O[C@H]2C(C)(C)[C@H](N)C2(C)C)C=C1Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231.  [Content Brief]