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Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).
Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level.
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
Apalutamide D4 (ARN-509 D4) is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
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