Androgen Receptor

Choose Selective Androgen Receptor Inhibitors

Androgen Receptor Signaling Pathway Map

Androgen Receptor Signaling Pathways

Androgen Receptor Products

  • All (48)
  • Androgen Receptor Inhibitors (11)
  • Androgen Receptor Antagonists (19)
  • Androgen Receptor Agonists (12)
  • Androgen Receptor Modulators (6)
  • New Androgen Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
S1123 Abiraterone (CB-7598) Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(16)3959
Sci Rep, 2021, 11(1):10765
S1195 TAK-700 (Orteronel) TAK-700 (Orteronel) 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.
Drug Metab Dispos, 2017, 45(6):635-645
Biochem Biophys Res Commun, 2016, 477(4):1005-10
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cancer Cell Int, 2020, 19;20:58
S1353 Ketoconazole (R 41400) Ketoconazole (R 41400) 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.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Nat Commun, 2021, 12(1):652
Pharmacol Res, 2021, 169:105648
S2246 Abiraterone Acetate (CB7630) Abiraterone Acetate (CB7630) 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.
Clin Cancer Res, 2021, clincanres.4391.2020
Neoplasia, 2021, 23(12):1261-1274
J Biol Chem, 2021, 297(2):100969
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.
J Pathol, 2021, 10.1002/path.5652
Nat Commun, 2020, 19;11(1):2508
Proc Natl Acad Sci U S A, 2020, 202021450
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.
S6965New ARV-110 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.
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.
S9667New CCS-1477 (CBP-IN-1) 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.
S1190 Bicalutamide (ICI-176334) Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Sci Adv, 2021, 7(27)eabg2564
Cell Rep, 2021, 36(10):109625
Cancer Lett, 2021, 520:172-183
S1250 Enzalutamide (MDV3100) Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Nat Med, 2021, 27(3):426-433
Nat Med, 2021, 10.1038/s41591-020-01168-7
J Extracell Vesicles, 2021, 10(10):e12136
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.
Cell Chem Biol, 2021, 28(6):788-801.e5
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
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
S2604 Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2
J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002
SSRN, 2021, 10.2139/ssrn.3886996
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.
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
Steroids, 2020, 153:108534
Steroids, 2018, 129:24-34
S4054 Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
Int J Mol Sci, 2021, 22(4)1638
J Biol Chem, 2021, S0021-9258(21)00252-0
J Environ Sci Health B, 2020, 55(2):91-102
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.
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
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.
S5285 RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
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.
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).
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.
Proc Natl Acad Sci U S A, 2020, 202021450
Mol Cancer Ther, 2020, molcanther.0417.2020
Mol Cancer Ther, 2020, 19;molcanther00152020
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Prostate, 2019, 79(2):206-214
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.
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.
S9898New 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.

S9900New 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.
S1140 Andarine Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
Drug Test Anal, 2020, 10.1002/dta.2917
J Am Soc Mass Spectrom, 2020, 31(11):2243-2249
S2832 Epiandrosterone Epiandrosterone (3β-androsterone, EpiA) is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
S3715 Boldenone Undecylenate Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.
S3717 Testosterone Enanthate Testosterone Enanthate (Testosterone heptanoate, NSC-17591) is an androgen and anabolic steroid used in androgen replacement therapy.
Cancers (Basel), 2021, 13(19)4937
Onco Targets Ther, 2020, 8;13:2987-2995
S3830 Protodioscin Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946 Mesterolone Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S4757 Dihydrotestosterone (DHT) Dihydrotestosterone (DHT, androstanolone, stanolone, 5α-DHT) is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.
Environ Health Perspect, 2021, 129(4):47010
Sci Rep, 2021, 11(1):14880
Prostate, 2021, 81(9):508-520
S4794 Drostanolone Propionate Drostanolone Propionate (Dromostanolone propionate, NSC-12198, Drostanolone 17β-propionate) is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795 Trenbolone acetate Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S5508 Dehydroepiandrosterone acetate Dehydroepiandrosterone acetate (DHEA, Androstenolone) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.
Br J Cancer, 2020, 10.1038/s41416-020-1007-3
Cancer Lett, 2016, 382(2):195-202
S6352 Androsterone Androsterone (5alpha-Androsterone) is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.
Mediators Inflamm, 2019, 2019:7162976
S6407 Tulobuterol hydrochloride Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.
S0276 GSK-2881078 GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
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
S1174 Ostarine (GTx-024) Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
J Clin Invest, 2021, 131(10)146777
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
Drug Test Anal, 2020, 10.1002/dta.2933
S5275 Testolone (RAD140) Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.
J Clin Invest, 2021, 131(10)146777
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
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.
S8822 Ligandrol (LGD-4033) Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity.
J Clin Invest, 2021, 131(10)146777
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
Anal Bioanal Chem, 2021, 10.1007/s00216-021-03740-7
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.
S1123 Abiraterone (CB-7598) Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(16)3959
Sci Rep, 2021, 11(1):10765
S1195 TAK-700 (Orteronel) TAK-700 (Orteronel) 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.
Drug Metab Dispos, 2017, 45(6):635-645
Biochem Biophys Res Commun, 2016, 477(4):1005-10
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cancer Cell Int, 2020, 19;20:58
S1353 Ketoconazole (R 41400) Ketoconazole (R 41400) 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.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Nat Commun, 2021, 12(1):652
Pharmacol Res, 2021, 169:105648
S2246 Abiraterone Acetate (CB7630) Abiraterone Acetate (CB7630) 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.
Clin Cancer Res, 2021, clincanres.4391.2020
Neoplasia, 2021, 23(12):1261-1274
J Biol Chem, 2021, 297(2):100969
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.
J Pathol, 2021, 10.1002/path.5652
Nat Commun, 2020, 19;11(1):2508
Proc Natl Acad Sci U S A, 2020, 202021450
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.
S6965New ARV-110 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.
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.
S9667New CCS-1477 (CBP-IN-1) 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.
S1190 Bicalutamide (ICI-176334) Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Sci Adv, 2021, 7(27)eabg2564
Cell Rep, 2021, 36(10):109625
Cancer Lett, 2021, 520:172-183
S1250 Enzalutamide (MDV3100) Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Nat Med, 2021, 27(3):426-433
Nat Med, 2021, 10.1038/s41591-020-01168-7
J Extracell Vesicles, 2021, 10(10):e12136
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.
Cell Chem Biol, 2021, 28(6):788-801.e5
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
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
S2604 Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2
J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002
SSRN, 2021, 10.2139/ssrn.3886996
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.
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
Steroids, 2020, 153:108534
Steroids, 2018, 129:24-34
S4054 Spironolactone Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
Int J Mol Sci, 2021, 22(4)1638
J Biol Chem, 2021, S0021-9258(21)00252-0
J Environ Sci Health B, 2020, 55(2):91-102
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.
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
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.
S5285 RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
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.
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).
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.
Proc Natl Acad Sci U S A, 2020, 202021450
Mol Cancer Ther, 2020, molcanther.0417.2020
Mol Cancer Ther, 2020, 19;molcanther00152020
S7955 EPI-001 EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Prostate, 2019, 79(2):206-214
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.
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.
S9898New 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.

S9900New 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.
S1140 Andarine Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
Drug Test Anal, 2020, 10.1002/dta.2917
J Am Soc Mass Spectrom, 2020, 31(11):2243-2249
S2832 Epiandrosterone Epiandrosterone (3β-androsterone, EpiA) is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
S3715 Boldenone Undecylenate Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.
S3717 Testosterone Enanthate Testosterone Enanthate (Testosterone heptanoate, NSC-17591) is an androgen and anabolic steroid used in androgen replacement therapy.
Cancers (Basel), 2021, 13(19)4937
Onco Targets Ther, 2020, 8;13:2987-2995
S3830 Protodioscin Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946 Mesterolone Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S4757 Dihydrotestosterone (DHT) Dihydrotestosterone (DHT, androstanolone, stanolone, 5α-DHT) is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.
Environ Health Perspect, 2021, 129(4):47010
Sci Rep, 2021, 11(1):14880
Prostate, 2021, 81(9):508-520
S4794 Drostanolone Propionate Drostanolone Propionate (Dromostanolone propionate, NSC-12198, Drostanolone 17β-propionate) is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795 Trenbolone acetate Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S5508 Dehydroepiandrosterone acetate Dehydroepiandrosterone acetate (DHEA, Androstenolone) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.
Br J Cancer, 2020, 10.1038/s41416-020-1007-3
Cancer Lett, 2016, 382(2):195-202
S6352 Androsterone Androsterone (5alpha-Androsterone) is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.
Mediators Inflamm, 2019, 2019:7162976
S6407 Tulobuterol hydrochloride Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.
S0276 GSK-2881078 GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
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
S1174 Ostarine (GTx-024) Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
J Clin Invest, 2021, 131(10)146777
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
Drug Test Anal, 2020, 10.1002/dta.2933
S5275 Testolone (RAD140) Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.
J Clin Invest, 2021, 131(10)146777
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
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.
S8822 Ligandrol (LGD-4033) Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity.
J Clin Invest, 2021, 131(10)146777
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
Anal Bioanal Chem, 2021, 10.1007/s00216-021-03740-7
S6965New ARV-110 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.
S9667New CCS-1477 (CBP-IN-1) 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.
S9898New 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.

S9900New 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.