Catalog No.
Product Name
Application
Product Information
Citations
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Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
- 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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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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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
- Soumitra Ghosh, .et al. , bioRxiv, 2023, Jun 28:2023.06.28.546870 PMID: 37425957
- Qian Liu, .et al. , Research Square, 2023, Mar 10
- 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
ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.- Syeda Afshan, .et al. , Cancer Med, 2024, Sep;13(18):e70240 PMID: 39300962
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Androgen receptor antagonist
MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.- Syeda Afshan, .et al. , Cancer Med, 2024, Sep;13(18):e70240 PMID: 39300962
- Shiv Verma, .et al. , Mol Carcinog, 2024, Jun;63(6):1051-1063 PMID: 38482990
- 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
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human AR (hAR) antagonist
ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct. -
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. -
CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
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. -
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 modulator
LGD-4033 is an investigational selective androgen receptor modulator for treatment of conditions such as muscle wasting and osteoporosis, currently under development by Ligand Pharmaceuticals. -
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) -
Androgen receptor antagonist
Nilutamide (Nilandron) is a non-steroidal anti-androgen drug proposed in the treatment of metastatic prostatic carcinoma. - 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. - 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. -
Androgen Receptor Inhibitor
SC428 is a selective androgen receptor (AR) inhibitor that targets the N-terminal domain, effectively reducing the transactivation of various isoforms including AR-V7, AR-v567es, and full-length AR (AR-FL) along with its LBD mutants. This compound inhibits the nuclear translocation, chromatin binding, and subsequent transcription of AR-regulated genes in response to androgens. Additionally, SC428 demonstrates significant anti-proliferative effects on tumor cells in vitro and promotes apoptosis in vivo, particularly in mice bearing 22RV1 xenografts. Its application in cancer research highlights its potential utility in targeting androgen-dependent tumors. -
Androgen Receptor PROTAC Degrader
PROTAC AR Degrader-8 is an androgen receptor (AR) PROTAC degrader that effectively induces degradation of full-length AR (AR-FL) with DC50 values of 0.018 μM in 22Rv1 cells and 0.14 μM in LNCaP cells, as well as degrading the AR-V7 variant with a DC50 of 0.026 μM in 22Rv1 cells. This compound exhibits potent inhibition of cancer cell proliferation, with IC50 values of 0.038 μM and 1.11 μM in 22Rv1 and LNCaP cells, respectively. PROTAC AR Degrader-8 induces G2/M cell cycle arrest and promotes apoptosis in 22Rv1 cells, demonstrating significant anticancer efficacy in both murine and zebrafish models. It is a valuable tool for investigating mechanisms underlying prostate cancer and castration-resistant prostate cancer. -
Androgen Receptor Antagonist
Deutenzalutamide-d3 is a deuterium-labeled analog of Enzalutamide, an androgen receptor (AR) antagonist. It exhibits potent activity with an IC50 of 36 nM in LNCaP prostate cancer cells. This reagent is valuable for studying androgen receptor signaling pathways and resistance mechanisms in prostate cancer research. -
Androgen Receptor Degrader
ZC9 is a novel androgen receptor (AR) degrader that directly binds to AR, inhibiting its Dihydrotestosterone-induced nuclear translocation. By promoting AR degradation through the ubiquitin-proteasome system, ZC9 effectively suppresses AR transcriptional activity, leading to a significant decrease in the mRNA levels of downstream genes such as PSA, TMPRSS2, and PMEPA1. Additionally, ZC9 induces apoptosis and demonstrates notable anticancer effects in prostate cancer models, making it a valuable tool for research in androgen signaling and cancer therapeutics. -
Androgen Receptor Antagonist
AR Antagonist 15 is an orally bioavailable antagonist of the androgen receptor (AR), exhibiting an IC50 of 97 nM for ART787A. This compound inhibits AR nuclear translocation, prevents AR homodimerization, and suppresses transcription of AR-regulated genes through competitive binding at the ligand binding pocket. Additionally, AR Antagonist 15 significantly reduces prostate-specific antigen (PSA) levels and induces apoptosis by decreasing the expression of proteins involved in apoptotic pathways. This reagent is relevant for studies investigating the mechanisms of prostate cancer. -
Androgen Receptor Inhibitor
Androgen receptor-IN-7 is a potent inhibitor of the androgen receptor (AR), demonstrating significant anticancer activity against PC-3 (IC50 = 370.37 nM) and LNCaP cell lines through both AR-dependent and AR-independent mechanisms. This compound induces reactive oxygen species (ROS) production in PC-3 cells, highlighting its potential role in oncological studies. Androgen receptor-IN-7 is useful for research focused on prostate cancer and related therapeutic strategies. -
Androgen Receptor Inhibitor
Ac-PPPHPHARIK-NH2 is an androgen receptor inhibitor that disrupts the interaction between the androgen receptor and Src. By preventing this binding, it effectively inhibits androgen or estrogen-induced receptor activation in cancer cells, thereby modulating related signaling pathways. This compound has been shown to impede cell cycle progression and suppress tumor growth, making it a valuable tool for research in cancer biology and hormone receptor signaling. -
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 Modulators
Ostarine is an androgen receptor modulator (SARM)
