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AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

GDC-2992 is a selective and oral AR (androgen receptor) degrader that inhibits the proliferation of tumor cells overexpressing AR, degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, and can be used for oncology studies in denuded resistant prostate cancer (CRPC).

VHL Ligand 8, a VHL ligand essential for synthesizing ARD-266, acts as a highly potent VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. It efficiently facilitates the degradation of AR protein in AR-positive prostate cancer cell lines LNCaP, VCaP, and 22Rv1, exhibiting DC50 values ranging from 0.2-1 nM [1].

Boc-Pip-alkyne-Ph-COOH, a PROTAC linker characterized by its alkyl ether composition, plays a crucial role in synthesizing PROTACs including ARD-266. This compound demonstrates significant efficacy in promoting the degradation of androgen receptor (AR) protein across AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, showcasing DC50 values ranging from 0.2-1 nM[1].

YJ1206 is a highly potent and selective CDK12 13 PROTAC degrader (IC50 =12.55 nM) with the advantages of oral administration and low toxicity, which triggers gene-length-dependent transcription elongation defects, leading to DNA damage and cell-cycle arrest, and inhibits the proliferation of a subpopulation of prostate cancer cells. YJ1206 can synergize with AKT pathway inhibitors to effectively inhibit prostate cancer.

PROTAC SMARCA2 degrader-26 (compound 45) is an effective degrader of SMARCA2 using the PROTAC technology. It induces degradation of SMARCA2 and SMARCA4 in VCaP cells, with degradation percentages of 94% and 57%, respectively. Additionally, PROTAC SMARCA2 degrader-26 demonstrates antiproliferative activity.

YJ9069 is a selective CDK12 CDK13P ROTAC degrader with an IC50 of 22.22 nM in VCaP cells. Rapid degradation of CDK12 13 by this compound triggers transcription elongation defects dependent on gene length, leading to DNA damage and cell cycle arrest. YJ9069 effectively inhibits the proliferation of prostate cancer cell subpopulations and significantly suppresses prostate tumor growth in vivo.

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

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.

ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of prostate cancer.

A031, a potent PROTAC androgen receptor (AR) degrader, demonstrates significant efficacy with an IC50 value under 0.25 μM for AR protein degradation. Additionally, it exhibits an inhibitory impact on tumor growth in zebrafish models of human prostate cancer (VCaP) [1].

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule from the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal domain (AR-NTD) of the Androgen Receptor variant AR-V7. By antagonizing AR-NTD, it effectively degrades AR-V7 protein and induces apoptosis in prostate cancer (PC) cells, with degradation efficiencies of 62.2% (1 μM) and 71.1% (5 μM) in VCaP cells [1].

ARD-2051 is a potent, orally active proteolysis-targeting chimera degrader of the androgen receptor (AR), exhibiting DC50 values of 0.6 nM in degrading AR protein within LNCaP and VCaP prostate cancer cell lines. It holds potential for prostate cancer research applications [1].

ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand. It demonstrates AR-degrading activity both in vitro and in vivo, and effectively inhibits VCaP tumor growth in mouse xenograft models [1].