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Androgen Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Int J Biol Macromol, 2024, 278(Pt 3):134844
Nat Struct Mol Biol, 2023, 30(12):1958-1969
Int J Mol Sci, 2023, 24(4)3823
S2803 Galeterone Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
ChemMedChem, 2022, e202200043
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
Steroids, 2020, 153:108534
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S2042 Cyproterone Acetate Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.
iScience, 2024, 27(10):110862
Sci Rep, 2021, 11(1):5457
Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332
Verified customer review of Cyproterone Acetate
S4728 3,3'-Diindolylmethane 3,3'-Diindolylmethane (DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. This compound is a strong, pure androgen receptor (AR) antagonist.
FASEB J, 2021, 35(5):e21502
Cell Death Dis, 2019, 10(2):38
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
S0839 ACP-105 ACP-105 is an orally available and potent selective androgen receptor modulator (SARM) with pEC50 of 9.0 and 9.4 for AR wild type and AR mutation T877A, respectively.
Drug Test Anal, 2020, 10.1002/dta.2917
S9898 Proxalutamide (GT0918)

Proxalutamide (GT0918), a second-generation androgen receptor antagonist, binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.
CNS Neurosci Ther, 2024, 30(6):e14822
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.
E1502 Deutenzalutamide Deutenzalutamide (HC-1119, MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. It can be used in a treatment of advanced prostate cancer.
S4836 Nilutamide Nilutamide (RU23908) is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.
S0276 GSK-2881078 GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
S4593 Chlormadinone acetate Chlormadinone acetate (Gestafortin) is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.
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.
S9900 JNJ-63576253 (TRC-253) JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM, and it displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of 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.
S8885 UT-34 UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. This compound is a potential next-generation therapeutic for -resistant prostate cancer.
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.
E1964 BMS-986365 BMS-986365 (CC-94676) is a potent and selective, heterobifunctional ligand-directed degrader (LDD) and antagonist of androgen receptor (AR), that effectively targets both wildtype and mutant forms of the androgen receptor (AR) in the cytoplasm and nucleus. It rapidly degrades AR, suppresses AR signaling, and shows promising clinical activity in inhibiting tumor growth in patients with metastatic castration-resistant prostate cancer (mCRPC).
E0608 Pyrilutamide (KX-826) Pyrilutamide (KX-826) is an antagonist of androgen receptor (AR) and a potential first-in-class topical drug for the treatment of androgenetic alopecia (AGA) and acne vulgaris.
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.
S9045 Triptophenolide Triptophenolide (Hypolide), derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
E2850 ORM-15341 ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 value of 38 nM and the inhibition constant (Ki) value of 8 nM.
S6896 Clascoterone Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) is a topical and peripherally selective antagonist of androgen receptor (AR).
E8049 Topilutamide Topilutamide is a topical nonsteroidal antiandrogen (NSAA) that is used in the treatment of metastatic prostate cancer.
S6630 Dimethylcurcumin (ASC-J9) Dimethylcurcumin (ASC-J9, Dimethyl curcumin, GO-Y025) is an androgen receptor (AR) degradation enhancer that suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
S5437 4,4'-DDE 4,4'-DDE (DDE, p,p'-DDE, p,p'-dichlorodiphenyldichloroethylene), a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.
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
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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
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.