19983-28-9

VPC-14228 is a specific inhibitor of AR-DBD. It acts by inhibiting both Y594A and Q592A mutants, blocking the interaction of the AR with androgen response elements in the nucleus..

VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer[1][2].

[1] Kush Dalal, et al. Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer. J Biol Chem. 2014 Sep 19;289(38):26417-26429. DOI:10.1074/jbc.M114.553818
[2] Bhumireddy A, et al. Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders. Bioorg Med Chem Lett. 2022 Jan 1;55:128448. DOI:10.1016/j.bmcl.2021.128448