ar-regulated

ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) that degrades the androgen receptor (AR), effectively reducing AR protein levels, suppressing AR-regulated gene expression in tumor tissues, and inhibiting tumor growth without evident toxicity. This compound holds promise for prostate cancer research.

SC428 acts as an inhibitor of the androgen receptor (AR), specifically targeting the N-terminal domain of AR. This compound effectively diminishes the transactivation of various AR forms, including AR-V7, ARv567es, full-length AR (AR-FL), and its LBD mutants. Additionally, SC428 significantly inhibits AR-FL nuclear translocation, chromatin binding, and AR-regulated gene transcription under androgen stimulation. In vitro, SC428 suppresses the proliferation of tumor cells. In vivo, it inhibits tumor growth in mice transplanted with 22Rv1 cells by inducing apoptosis.

AR antagonist 15 is an orally active androgen receptor (AR) antagonist with an IC50 of 97 nM for ART787A. It impairs AR nuclear translocation, hinders AR homodimerization, and inhibits AR-regulated gene transcription by competitively binding to the ligand-binding pocket. AR antagonist 15 significantly reduces prostate-specific antigen (PSA) levels and induces apoptosis by decreasing the expression of apoptosis-related proteins. This compound is useful for prostate cancer research.

Y08060 is an effective and selective BET Inhibitor for the Treatment of Prostate Cancer. Y08060 effectively suppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC in prostate cancer cell lines. Y08060 has IC50 values of 3.23 and 4.41 μM in inhibition of cell viability in the C4 2B and LNCaP cell lines, respectively.

ARD-69 is a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent mann