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, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
-
Prostate, 2022, 82(3):314-322
-
J Pathol, 2021, 10.1002/path.5652
-
Nat Commun, 2020, 19;11(1):2508
|
|
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 |
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. |
|
|
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. |
|
|
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. |
|
|
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. |
-
Cell Commun Signal, 2022, 20(1):31
-
Sci Adv, 2021, 7(27)eabg2564
-
Cell Rep, 2021, 36(10):109625
|
|
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. |
-
Sci Adv, 2022, 8(17):eabh3635
-
Cancer Res, 2022, canres.1807.2021
-
NPJ Precis Oncol, 2022, 6(1):21
|
|
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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Chem Biol, 2021, 28(6):788-801.e5
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
-
ChemMedChem, 2022, e202200043
-
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
-
Steroids, 2020, 153:108534
|
|
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.
|
-
J Med Chem, 2022, 65(3):2507-2521
-
Life Sci Alliance, 2022, 5(4)e202101116
-
J Oncol, 2022, 2022:6085948
|
|
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. |
-
Int J Mol Sci, 2022, 23(8)4404
-
J Clin Invest, 2021, 131(10)146777
-
Anal Chem, 2021, 10.1021/acs.analchem.1c01083
|
|
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, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
- Prostate, 2022, 82(3):314-322
- J Pathol, 2021, 10.1002/path.5652
- Nat Commun, 2020, 19;11(1):2508
|
|
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 |
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. |
|
|
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. |
|
|
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. |
|
|
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. |
- Cell Commun Signal, 2022, 20(1):31
- Sci Adv, 2021, 7(27)eabg2564
- Cell Rep, 2021, 36(10):109625
|
|
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. |
- Sci Adv, 2022, 8(17):eabh3635
- Cancer Res, 2022, canres.1807.2021
- NPJ Precis Oncol, 2022, 6(1):21
|
|
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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Chem Biol, 2021, 28(6):788-801.e5
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
|
|
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. |
- ChemMedChem, 2022, e202200043
- Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
- Steroids, 2020, 153:108534
|
|
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. |
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S9898New |
Proxalutamide (GT0918)
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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.
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S9900New |
JNJ-63576253 (TRC-253)
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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. |
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S1140 |
Andarine
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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
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S2832 |
Epiandrosterone
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Epiandrosterone (3β-androsterone, EpiA) is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA. |
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S3715 |
Boldenone Undecylenate
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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. |
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S3717 |
Testosterone Enanthate
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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
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S3830 |
Protodioscin
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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. |
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S3946 |
Mesterolone
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Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities. |
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S4757 |
Dihydrotestosterone (DHT)
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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.
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- J Med Chem, 2022, 65(3):2507-2521
- Life Sci Alliance, 2022, 5(4)e202101116
- J Oncol, 2022, 2022:6085948
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S4794 |
Drostanolone Propionate
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Drostanolone Propionate (Dromostanolone propionate, NSC-12198, Drostanolone 17β-propionate) is an anabolic androgenic steroid with strong anti-estrogenic properties. |
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S4795 |
Trenbolone acetate
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Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone. |
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S5508 |
Dehydroepiandrosterone acetate
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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
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S6352 |
Androsterone
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Androsterone (5alpha-Androsterone) is a steroid metabolite derived from sex hormones, which displays weak androgenic properties. |
- Mediators Inflamm, 2019, 2019:7162976
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S6407 |
Tulobuterol hydrochloride
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Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities. |
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