Catalog No.
Product Name
Application
Product Information
Product Citation
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Androgen Receptor antagonist
(R)-Bicalutamide is an active competitive non-steroidal androgen receptor antagonist with an IC50 of 0.17 μM for MDA 453 cells. -
Androgen antagonist
17 alpha-propionate is a new topical and peripherally selective androgen antagonist. -
Androgen Receptor agonist
Andarine (GTX-007) is an investigational selective androgen receptor modulator (SARM). -
Androgen Receptor antagonist
Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.- Mirielle C Nauman, .et al. , Cancers (Basel), 2023, Apr 1;15(7):2118 PMID: 37046780
- Mi Chen, .et al. , EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. , Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Androgen Receptor Modulators
Ostarine is an androgen receptor modulator (SARM) -
Androgen receptor antagonist
MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.- Shiv Verma, .et al. , Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. , EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. , Mol Carcinog, 2021, Dec 22 PMID: 34939235
- Megestrol Acetate is a progesterone derivative with antineoplastic properties
- Hong Wang, .et al. , Exp Biol Med (Maywood), 2021, Jul 7 PMID: 34233525
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CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. - ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
- Ruibao Chen, .et al. , Biomed Res Int., 2015, 2015: 514234 PMID: 26491675
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Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. -
AR inhibitor downregulator
AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.- Qian Liu, .et al. , Nat Commun, 2024, Feb 7;15(1):1148 PMID: 38326303
- Qian Liu, .et al. , Research Square, 2023, Mar 10
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androgen receptor modulator
GSK-2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. - Bopindolol malonate is a non-selective, potent, long-acting beta adrenoceptor antagonist. It demonstrates inhibition of H2O2-induced lipid peroxdiation.
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CYP17A1/androgen synthesis inhibitor
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues. -
androgen-receptor (AR) antagonist
N-desMethyl EnzalutaMide is used in the treatment of disorders involving androgen, estrogen and progesterone receptors. -
Androgen Receptor antagonist
EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ?? 6 μM) - Androsterone is a steroid hormone produced in the body from 5α-reduced metabolites of dehydroepiandrosterone. It is the major androgen excreted in urine as a metabolite of testosterone and is used as the international reference standard for androgenic activity.
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Androgen receptor antagonist
Spironolactone is a potent antagonist of the androgen receptor. -
OC2 inhibitor
CSRM617 Hydrochloride is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice. - 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
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AR antagonist
Proxalutamide (GT0918) is a potent androgen receptor (AR) antagonist. -
androgen ligand
Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs. -
CB1 agonist
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. -
androgen receptor antagonist
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor. -
Androgen receptor antagonist
Nilutamide (Nilandron) is a non-steroidal anti-androgen drug proposed in the treatment of metastatic prostatic carcinoma. -
SARD ligand
(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer. -
Antiandrogenic agent
4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. -
Androgen receptor antagonist
TRC253, also known as JNJ63576253, is a potent and orally active androgen receptor antagonist.
