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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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) -
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. -
PROTAC Androgen Receptor Degrader
ARD-266 is a potent PROTAC degrader targeting the Androgen Receptor (AR) through a von Hippel-Lindau E3 ligase mechanism. It effectively induces AR protein degradation in AR-positive prostate cancer cell lines, including LNCaP, VCaP, and 22Rv1, with DC50 values ranging from 0.2 to 1 nM. Additionally, ARD-266 features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating versatile applications in chemical biology research. -
PROTAC AR Degrader
ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand. -
PROTAC
Luxdegalutamide (ARV-766) is an orally active proteolysis-targeting chimera (PROTAC) designed to selectively degrade the androgen receptor (AR), including clinically relevant resistance-associated mutants such as T878A, H875Y, and L702H. By inducing AR ubiquitination and proteasomal degradation, Luxdegalutamide effectively suppresses AR signaling and exhibits potent antitumor activity. It is a promising therapeutic agent and research tool for studying castration-resistant prostate cancer (CRPC) and mechanisms of AR-driven oncogenesis. -
PROTAC AR/AR-V7 degrader
PROTAC AR/AR-V7 Degrader-1 (27c) is a PROTAC-based dual degrader targeting both full-length androgen receptor (AR) and its splice variant AR-V7, which is implicated in resistance to androgen deprivation therapies. It exhibits DC₅₀ values of 2.67 μM for AR and 2.64 μM for AR-V7, effectively promoting their proteasomal degradation. By eliminating both isoforms, compound 27c induces apoptosis in AR-driven cancer cells, making it a promising therapeutic candidate for castration-resistant prostate cancer (CRPC) and other AR/AR-V7–dependent malignancies. -
PROTAC AR degrader
ARD-1676 is an orally bioavailable PROTAC degrader of the androgen receptor (AR), composed of an AR-binding ligand and a cereblon-recruiting moiety. It effectively induces AR degradation both in vitro and in vivo, and demonstrates significant antitumor activity by inhibiting VCaP prostate cancer xenograft growth in mouse models. ARD-1676 represents a promising therapeutic strategy for targeting AR-driven malignancies. -
PROTAC AR degrader
ARD-61 is a highly potent and selective PROTAC degrader of the androgen receptor (AR), also capable of degrading progesterone receptors (PR) in AR-positive cancer cell lines. It induces apoptosis and demonstrates significant antitumor efficacy in vivo, effectively inhibiting tumor growth in the MDA-MB-453 xenograft mouse model. Additionally, ARD-61 is equipped with an alkyne functional group, enabling its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, facilitating conjugation and functionalization for chemical biology applications. -
PROTAC AR Degrader
ARD-2128 is a highly potent, orally bioavailable PROTAC degrader targeting the androgen receptor (AR). It efficiently reduces AR protein levels, downregulates AR-regulated gene expression in tumor tissues, and inhibits tumor growth without observable toxicity. ARD-2128 is a promising tool for prostate cancer research. -
PROTAC AR-V7 degrader
MTX-23 is an androgen receptor (AR)-targeting PROTAC that degrades both AR-FL and the splice variant AR-V7. It effectively inhibits prostate cancer cell proliferation and induces apoptosis, making it a promising tool for studying AR signaling and therapeutic resistance in prostate cancer. -
androgen receptor (AR) PROTAC degrader
BMS-986365 (CC-94676) is an orally active, selective PROTAC degrader targeting the androgen receptor (AR), including AR mutants. It functions via cereblon (CRBN)-mediated ubiquitination and proteasomal degradation of AR. BMS-986365 exhibits strong in vivo efficacy by suppressing AR signaling and inhibiting tumor growth in advanced prostate cancer models, making it a promising candidate for therapeutic development. -
androgen receptor (AR) PROTAC degrader
Bavdegalutamide (ARV-110) is an orally active and highly specific PROTAC degrader targeting the androgen receptor (AR). It induces ubiquitination and proteasomal degradation of AR, offering a novel therapeutic approach for AR-driven diseases such as prostate cancer. -
Androgen Receptor (AR) degrader
ARCC-4 is a low-nanomolar PROTAC degrader targeting the androgen receptor (AR), with a DC₅₀ of 5 nM. Based on enzalutamide and incorporating a von Hippel-Lindau (VHL) E3 ligase ligand, ARCC-4 efficiently degrades both wild-type and clinically relevant AR mutants linked to resistance to antiandrogen therapy. It outperforms enzalutamide in potency and degradation efficacy, making it a promising candidate for advanced prostate cancer research. -
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 Antagonist
Atraric acid, known as Methyl atrarate, functions as a specific antagonist of androgen receptors (AR). This compound demonstrates significant anti-inflammatory and anticancer properties by downregulating the expression of the prostate-specific antigen gene in LNCaP and C4-2 cell lines. Additionally, atraric acid inhibits nitric oxide synthesis and cytokine production while suppressing the MAPK-NFκB signaling pathway. Its utility in research extends to investigations of prostate diseases and inflammatory conditions. -
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. -
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. - 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 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.
