Androgen Receptor

Androgen Receptor Products

  • All (37)
  • Androgen Receptor Inhibitors (13)
  • Androgen Receptor Antagonists (21)
  • Androgen Receptor Modulators (3)
  • New Androgen Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1250 Enzalutamide Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Cancers (Basel), 2024, 16(2)296
bioRxiv, 2024, 10.1101/2024.01.16.575611
bioRxiv, 2024, 10.1101/2023.12.01.569685
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Cancers (Basel), 2024, 16(2)296
Biomedicines, 2024, 12(1)181
J Exp Clin Cancer Res, 2023, 42(1):204
S1123 Abiraterone Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) 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
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.
Cancer Res, 2023, 83(2):219-238
J Immunother Cancer, 2023, 11(5)e006581
Pharmacol Res, 2023, 189:106692
S2840 Apalutamide (ARN-509) Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
Oncogene, 2024, 43(4):235-247
Nat Commun, 2023, 14(1):5253
Nat Commun, 2023, 14(1):5253
S1353 Ketoconazole Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.
J Med Virol, 2023, 95(6):e28856
Cell Death Dis, 2023, 14(1):64
Cell Death Dis, 2023, 14(8):488
S1908 Flutamide Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
Int J Mol Sci, 2022, 23-169390
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7559 Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
Nat Commun, 2023, 14(1):5253
Nat Commun, 2023, 14(1):5253
Cancer Res, 2023, 83(3):456-470
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S4054 Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
J Cell Mol Med, 2023, 27(8):1069-1082
ESC Heart Fail, 2022, 10.1002/ehf2.14186
Int J Mol Sci, 2021, 22(4)1638
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
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 Mol Sci, 2023, 24(4)3823
Cell Death Dis, 2022, 13(7):626
Mar Drugs, 2022, 20(6)378
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). TAK-700 (Orteronel) 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
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.
Sci Rep, 2021, 11(1):5457
Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332
S4728 3,3'-Diindolylmethane 3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
FASEB J, 2021, 35(5):e21502
Cell Death Dis, 2019, 10(2):38
S6965 Bavdegalutamide (ARV-110) Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. ARV-110 completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM. ARV-110 can be used for the research of prostate cancer.
Nucleic Acids Res, 2023, gkad642
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
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.
E1502New 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.
S9900 JNJ-63576253 (TRC-253) JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.
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. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.
S5285 RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
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.
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.
E0608New 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.
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. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone 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
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.
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.
S9898 Proxalutamide (GT0918)

Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.

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).
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.
S1123 Abiraterone Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) 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
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.
Cancer Res, 2023, 83(2):219-238
J Immunother Cancer, 2023, 11(5)e006581
Pharmacol Res, 2023, 189:106692
S2840 Apalutamide (ARN-509) Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
Oncogene, 2024, 43(4):235-247
Nat Commun, 2023, 14(1):5253
Nat Commun, 2023, 14(1):5253
S1353 Ketoconazole Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.
J Med Virol, 2023, 95(6):e28856
Cell Death Dis, 2023, 14(1):64
Cell Death Dis, 2023, 14(8):488
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
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). TAK-700 (Orteronel) 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
S6965 Bavdegalutamide (ARV-110) Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. ARV-110 completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM. ARV-110 can be used for the research of prostate cancer.
Nucleic Acids Res, 2023, gkad642
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.
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.
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.
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.
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. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone 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
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.
S1250 Enzalutamide Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Cancers (Basel), 2024, 16(2)296
bioRxiv, 2024, 10.1101/2024.01.16.575611
bioRxiv, 2024, 10.1101/2023.12.01.569685
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Cancers (Basel), 2024, 16(2)296
Biomedicines, 2024, 12(1)181
J Exp Clin Cancer Res, 2023, 42(1):204
S1908 Flutamide Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
Int J Mol Sci, 2022, 23-169390
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7559 Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
Nat Commun, 2023, 14(1):5253
Nat Commun, 2023, 14(1):5253
Cancer Res, 2023, 83(3):456-470
S4054 Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
J Cell Mol Med, 2023, 27(8):1069-1082
ESC Heart Fail, 2022, 10.1002/ehf2.14186
Int J Mol Sci, 2021, 22(4)1638
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
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 Mol Sci, 2023, 24(4)3823
Cell Death Dis, 2022, 13(7):626
Mar Drugs, 2022, 20(6)378
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.
Sci Rep, 2021, 11(1):5457
Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332
S4728 3,3'-Diindolylmethane 3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
FASEB J, 2021, 35(5):e21502
Cell Death Dis, 2019, 10(2):38
E1502New 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.
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.
S9900 JNJ-63576253 (TRC-253) JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.
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. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.
S5285 RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
E0608New 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.
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.
S9898 Proxalutamide (GT0918)

Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.

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).
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.
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
S0276 GSK-2881078 GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
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.
E1502New 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.
E0608New 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.

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