CYP17A1 Inhibitor

4-Pyridylmethyl adamantanecarboxamide (Compound 11) is an Aromatase inhibitor with an IC₅₀ of 1.5 μM against hAromatase. 4-Pyridylmethyl adamantanecarboxamide inhibits the C17,20-lyase activity of testicular cytochrome P450_17α with an IC₅₀ of 1600 nM, and also inhibits the 17α-hydroxylase activity of this enzyme with an IC₅₀ of 7700 nM. 4-Pyridylmethyl adamantanecarboxamide can be used in the research of prostate cancer.

CYP17A1/HDAC6-IN-1 (compound 12) is a potent inhibitor of CYP17A1/HDAC6, with IC₅₀ of 0.284μM and 0.6015 μM,respectively. CYP17A1/HDAC6-IN-1 has anti-tumor activity.

YXG‑158 is an orally active, anticancer bifunctional steroid analog with both androgen receptor (AR) degradation activity (DC₅₀ = 1.28 μM) and CYP17A1 inhibitory activity (IC₅₀ = 100 nM). YXG-158 reduces AR protein and mRNA expression via proteasome-dependent degradation, degrades AR-V7, and inhibits CYP17A1 enzymatic activity to block androgen biosynthesis. YXG-158 inhibits the activities of ERα and ERβ, as well as cancer cell proliferation. YXG-158 decreases the weight of androgen-sensitive organs in castrated rats treated with testosterone propionate, downregulates AR protein, reduces PSA levels, and suppresses tumor growth in Enzalutamide (HY-70002)-sensitive and -resistant xenograft models. YXG-158 can be used in prostate cancer-related research.

ASN-001 is an orally active CYP-17A1 lyase inhibitor that selectively inhibits testosterone synthesis. ASN-001 has anticancer activity and can be used for research in the field of prostate cancer.

CYP17A1-IN-2 is a potent inhibitor of CYP17A1. CYP17A1-IN-2 exhibits anti-proliferative activity against prostate cancer cells. CYP17A1-IN-2 can be used in research related to castration-resistant prostate cancer.