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Androgen Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. This compound triggers DNA damage characterized by activation of the ATM/ATR pathway. It induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. This chemical is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
Theranostics, 2024, 14(4):1371-1389
Theranostics, 2024, 1371-1389
S7040 AZD3514 AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
E8277New GDC-2992 GDC-2992 (RO7656594, Compound 28A) is an orally active degrader of androgen receptor (AR) with a DC50 of 2.7 nM. It binds to AR and cereblon (CRBN), inducing AR ubiquitination and degradation. This compound also inhibits cell proliferation in VCaP cells and exhibits potential to reduce treatment resistance and disease relapse in prostate cancer.
E8283New ID11916 ID11916 is an orally available antagonist of Androgen receptor (AR) that blocks androgen binding, AR nuclear translocation, and transcriptional activity. It also inhibits PDE5 and exhibits anti-proliferative activity. This compound inhibits tumor growth in the MDA-MB-453 xenograft model.
E8305New ATC-324 ATC-324 is a potent AUTOphagy-TArgeting Chimera (AUTOTAC) degrader of androgen receptor (AR) with a DC50 of 2.05 µM. It induces autophagy–lysosomal degradation of AR, reduces nuclear AR and AR-V7 activity, and causes cytotoxicity in AR-positive prostate cancer cells, making it useful for prostate cancer research.
E0377 CLP-3094 CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
S3542 N-desMethyl EnzalutaMide N-desMethyl EnzalutaMide (N-desmethyl MDV 3100) is the active metabolite of Enzalutamide, which is an oral androgen receptor inhibitor for treatment of castration-resistant prostate cancer.
S2246 Abiraterone Acetate Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor.
Adv Sci (Weinh), 2025, 12(31):e01284
Cancer Med, 2025, 14(9):e70855
Cells, 2024, 13(19)1622
Verified customer review of Abiraterone Acetate
S1123 Abiraterone Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. This compound is an androgen biosynthesis inhibitor.
Cancer Res, 2023, 83(8):1361-1380
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(16)3959
Verified customer review of Abiraterone
S1353 Ketoconazole Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. This compound is an androgen biosynthesis inhibitor.
Nature, 2025, 10.1038/s41586-025-09755-9
Mol Oncol, 2025, 10.1002/1878-0261.13799
Discov Oncol, 2024, 15(1):709
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
iScience, 2024, 27(10):110862
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Verified customer review of Megestrol Acetate
S9667 Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
Nat Genet, 2025, 57(10):2468-2481
Nat Commun, 2025, 16(1):4133
PLoS Pathog, 2025, 21(9):e1013073
S1195 Orteronel Orteronel(TAK-700) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). This compound is an androgen biosynthesis inhibitor. Phase 3.
Toxicol Appl Pharmacol, 2023, 475:116638
Drug Metab Dispos, 2017, 45(6):635-645
Biochem Biophys Res Commun, 2016, 477(4):1005-10
S0097 (S,R,S)-AHPC (MDK7526) (S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor. (S,R,S)-AHPC can be connected to the ligand for protein such as BCR-ABL1 by a linker to form PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells.