Androgen Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Androgen Receptor Products

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cancers (Basel), 2021, 13(16)3959 Sci Rep, 2021, 11(1):10765 J Biol Chem, 2021, 297(2):100969	Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
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 J Biol Chem, 2021, 297(2):100969 Mol Cancer Ther, 2020, 19;molcanther00152020	BCaPT10 and BPH-1 cells were treated with vehicle (NTC, white bars), 10 uM abiraterone (ABI, gray bars), or abiraterone plus steroid hormones (black bars, 100 nM DHT, 10 nM estradiol, and 10 nM progestin). Minimum of 200 cells per condition was used from each of at least 3 independent experiments. Each result is shown as the average 盨EM from at least 3 independent experiments. One-way ANOVA. , P < .05; , P < .01; , P < .005; **, P < .001.
S6965^New	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.
S9667^New	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.
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	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
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
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/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514 is a potent and oral androgen receptor downregulator with K_i of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
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.
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, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
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
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	Immunohistochemical staining of Ki67 was performed to determine cell proliferation in the tumors. Each tissue section was counted manually in three different areas to assess the Ki67-positive cell index. Data were then presented as number of Ki67-positive cells per x 400 microscope field. Results are presented as the means s.d. **P < 0.001 by Student 's t-test, compared with control.
S9900^New	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.
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	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i 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/s13577-021-00579-z J Am Heart Assoc, 2020, 9(20):e015773	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
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 SSRN, 2021, 10.2139/ssrn.3886996 Elife, 2020, 9e56749
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	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
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	(h and i) Triptolide inhibits transcription. After exposure to triptolide (1 μm), spironolactone (10 μm), actinomycin D (2 μm, transcription inhibitor used as a positive control) or DMSO for 6 h, the global RNA synthesis was evaluated by the measurement of 5-EU incorporation. The figure shows representative merged pictures of DAPI and 5-EU signal. The intensity of the signal was evaluated through fluorescence microscopy (h) and quantified with the CellProfiler Software. Triptolide but not spironolactone inhibits global transcription.
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.
S7559	Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i 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	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
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.
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
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.
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).
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
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.
S1140	Andarine Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with K_i 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.
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.
S6352	Androsterone Androsterone (5alpha-Androsterone) is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.	Mediators Inflamm, 2019, 2019:7162976
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
S3946	Mesterolone Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S6407	Tulobuterol hydrochloride Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.
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.
S3717	Testosterone Enanthate Testosterone Enanthate (Testosterone heptanoate, NSC-17591) is an androgen and anabolic steroid used in androgen replacement therapy.	Onco Targets Ther, 2020, 8;13:2987-2995
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.
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
S1174	Ostarine (GTx-024) Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with K_i 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
S0276	GSK-2881078 GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
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
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
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.

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cancers (Basel), 2021, 13(16)3959 Sci Rep, 2021, 11(1):10765 J Biol Chem, 2021, 297(2):100969	Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
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 J Biol Chem, 2021, 297(2):100969 Mol Cancer Ther, 2020, 19;molcanther00152020	BCaPT10 and BPH-1 cells were treated with vehicle (NTC, white bars), 10 uM abiraterone (ABI, gray bars), or abiraterone plus steroid hormones (black bars, 100 nM DHT, 10 nM estradiol, and 10 nM progestin). Minimum of 200 cells per condition was used from each of at least 3 independent experiments. Each result is shown as the average 盨EM from at least 3 independent experiments. One-way ANOVA. , P < .05; , P < .01; , P < .005; **, P < .001.
S6965^New	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.
S9667^New	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.
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	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
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
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/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514 is a potent and oral androgen receptor downregulator with K_i of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
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.
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, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.

Catalog No.	Information	Product Use Citations	Product Validations
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
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	Immunohistochemical staining of Ki67 was performed to determine cell proliferation in the tumors. Each tissue section was counted manually in three different areas to assess the Ki67-positive cell index. Data were then presented as number of Ki67-positive cells per x 400 microscope field. Results are presented as the means s.d. **P < 0.001 by Student 's t-test, compared with control.
S9900^New	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.
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	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i 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/s13577-021-00579-z J Am Heart Assoc, 2020, 9(20):e015773	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
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 SSRN, 2021, 10.2139/ssrn.3886996 Elife, 2020, 9e56749
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	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
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	(h and i) Triptolide inhibits transcription. After exposure to triptolide (1 μm), spironolactone (10 μm), actinomycin D (2 μm, transcription inhibitor used as a positive control) or DMSO for 6 h, the global RNA synthesis was evaluated by the measurement of 5-EU incorporation. The figure shows representative merged pictures of DAPI and 5-EU signal. The intensity of the signal was evaluated through fluorescence microscopy (h) and quantified with the CellProfiler Software. Triptolide but not spironolactone inhibits global transcription.
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.
S7559	Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i 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	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
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.
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
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.
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).
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
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.

Catalog No.	Information	Product Use Citations
S1140	Andarine Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with K_i 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.
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.
S6352	Androsterone Androsterone (5alpha-Androsterone) is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.	Mediators Inflamm, 2019, 2019:7162976
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
S3946	Mesterolone Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S6407	Tulobuterol hydrochloride Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.
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.
S3717	Testosterone Enanthate Testosterone Enanthate (Testosterone heptanoate, NSC-17591) is an androgen and anabolic steroid used in androgen replacement therapy.	Onco Targets Ther, 2020, 8;13:2987-2995
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.
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

Catalog No.	Information	Product Use Citations
S1174	Ostarine (GTx-024) Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with K_i 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
S0276	GSK-2881078 GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
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
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
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.

Choose Your Country or Region

By Signaling Pathways

By product type

Androgen Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Androgen Receptor Products