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androgen receptor (AR) antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (92) 5 alpha Reductase (1) Apoptosis (5) Aryl Hydrocarbon Receptor (3) Autophagy (9) Bacterial (1) Bcl-2 Family (2) Caspase (2) Drug Isomer (1) Drug Metabolite (3) Environmental Pollutants (3) Estrogen Receptor/ERR (6) Fungal (3) Glucocorticoid Receptor (3) Herbicide (1) Isotope-Labeled Compounds (12) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (3) Mineralocorticoid Receptor (7) NF-κB (2) NO Synthase (2) p38 MAPK (2) Phosphodiesterase (PDE) (1) Progesterone Receptor (1) Prostaglandin Receptor (1) PROTACs (2) Pyroptosis (2) Reference Standards (12)
By Research Areas:	Cancer (83) Cardiovascular Disease (7) Endocrinology (17) Infection (5) Inflammation/Immunology (7) Metabolic Disease (6) Neurological Disease (2)
Click Chemistry:	PROTAC Synthesis (1)

106

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-70002

Enzalutamide Maximum Cited Publications 214 Publications Verification MDV3100	Androgen Receptor Autophagy	Cancer
Enzalutamide (MDV3100) is an **androgen receptor (AR)** antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .

HY-16985

Darolutamide 5+ Cited Publications ODM-201; BAY-1841788	Androgen Receptor	Cancer
Darolutamide (ODM-201) is an orally active competitive **androgen receptor (AR)** antagonist. Darolutamide has a K_i of 11 nM for rat wild-type AR (wtAR) and IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-111372

Finerenone 5+ Cited Publications BAY 94-8862	Mineralocorticoid Receptor	Cardiovascular Disease Metabolic Disease
Finerenone (BAY 94-8862) is a third-generation, selective, and orally active nonsteroidal *mineralocorticoid receptor* (MR)** antagonist (IC₅₀ = 18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (> 500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-16060

Apalutamide 10+ Cited Publications ARN-509	Androgen Receptor	Cancer
Apalutamide (ARN-509) is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-14249

Bicalutamide 15+ Cited Publications	Androgen Receptor Autophagy	Cancer
Bicalutamide is an orally active non-steroidal **androgen receptor (AR)** antagonist. Bicalutamide can be used for the research of prostate cancer .

HY-15758

3,3'-Diindolylmethane 10+ Cited Publications DIM; Arundine; HB 236	Androgen Receptor Autophagy	Cancer
3,3'-Diindolylmethane is a strong, pure **androgen receptor** (AR) antagonist.

HY-B0845

Prochloraz 1 Publications Verification BTS 40542	Environmental Pollutants Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Fungal Androgen Receptor	Infection Endocrinology
Prochloraz is an imidazole antifungal. Prochloraz is as an *estrogen receptor* (ER) and androgen receptor (AR)** antagonist and an aromatase inhibitor with IC₅₀ values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the *aryl hydrocarbon receptor* (AhR) having an EC₅₀** of 1 μM .

HY-100186

GSK-2881078 5 Publications Verification	Androgen Receptor	Cardiovascular Disease Others Metabolic Disease Inflammation/Immunology Endocrinology Cancer
GSK-2881078 is an orally active and nonsteroidal selective **androgen receptor** modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)₂ cells (EC₅₀ = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .

HY-N2908

Atraric acid Methyl atrarate	Environmental Pollutants NF-κB Androgen Receptor p38 MAPK NO Synthase	Inflammation/Immunology Cancer
Atraric acid (Methyl atrarate) is a specific **androgen receptor (AR)** antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .

HY-111372R

Finerenone (Standard) BAY 94-8862 (Standard)	Reference Standards Mineralocorticoid Receptor	Cardiovascular Disease
Finerenone (Standard) is the analytical standard of Finerenone. This product is intended for research and analytical applications. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal *mineralocorticoid receptor* (MR)** antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-70002B

Enzalutamide carboxylic acid 2 Publications Verification MDV3100 carboxylic acid	Drug Metabolite	Cancer
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist .

HY-130845A

AR antagonist 1 hydrochloride	Ligands for E3 Ligase Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
AR antagonist 1 (compound 29) hydrochloride is a potent **androgen receptor (AR)** antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020) .

HY-70002R

Enzalutamide (Standard) MDV3100 (Standard)	Reference Standards Androgen Receptor Autophagy	Cancer
Enzalutamide (Standard) is the analytical standard of Enzalutamide. This product is intended for research and analytical applications. Enzalutamide (MDV3100) is an **androgen receptor (AR)** antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .

HY-130992

Androgen receptor antagonist 1	Androgen Receptor Ligands for Target Protein for PROTAC	Cancer
Androgen receptor antagonist 1 is an orally available full **androgen receptor** (AR) antagonist with an IC₅₀ of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .

HY-19337

Ketodarolutamide 1 Publications Verification BAY 1896953; ORM-15341	Androgen Receptor	Cancer
Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of **androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀** value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .

HY-112895

UT-155 2 Publications Verification	Androgen Receptor	Cancer
UT-155 is a selective and potent androgen receptor *(AR)* antagonist, with a K_i of 267 nM for UT-155 binding to AR-LBD.

HY-109070

Ralaniten EPI-002	Androgen Receptor	Cancer
Ralaniten (EPI-002) is a potent and orally active antagonist of the **androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC₅₀** of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .

HY-70002S1

Enzalutamide-d6 MDV3100-d₆	Isotope-Labeled Compounds Androgen Receptor	Cancer
Enzalutamide-d₆ (MDV3100-d₆) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells .

HY-136242

UT-34	Estrogen Receptor/ERR	Endocrinology Cancer
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, *F876L-AR, and W741L-AR*, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

HY-B1866

Linuron 1 Publications Verification	Environmental Pollutants Androgen Receptor Herbicide	Infection Metabolic Disease Cancer
Linuron is a phenylurea herbicide widely used to control the growth of grasses and weeds in various crops and orchards. Linuron acts as a photosystem II inhibitor. It also functions as a competitive androgen receptor (AR) antagonist, with an EC₅₀ of 200 μM and a K_i of 100 μM against rat AR, and an EC₅₀ of 20 μM against human AR. Linuron exhibits reproductive toxicity in animals and acts as an endocrine disruptor .\n

HY-114402

ARD-69	PROTACs Androgen Receptor	Cancer
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

HY-70002S

Deutenzalutamide Enzalutamide-d₃; MDV3100-d₃	Androgen Receptor Autophagy	Cancer
Deutenzalutamide (Enzalutamide-d₃) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .

HY-150102

EPI-7170 1 Publications Verification	Androgen Receptor	Cancer
EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .

HY-108250

(R)-Bicalutamide	Androgen Receptor	Cancer
(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an **androgen receptor (AR)** antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .

HY-115282A

JNJ-63576253 1 Publications Verification TRC-253	Androgen Receptor	Cancer
JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of **androgen receptor (AR), with IC₅₀**s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .

HY-N0475

Triptophenolide Hypolide; (+)-Triptophenolide	Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis	Inflammation/Immunology Cancer
Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC₅₀ of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .

HY-15758R

3,3'-Diindolylmethane (Standard) DIM (Standard); Arundine (Standard); HB 236 (Standard)	Reference Standards Androgen Receptor Autophagy	Cancer
3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.

HY-141487

CLP-3094 2 Publications Verification	Androgen Receptor	Metabolic Disease Inflammation/Immunology
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the **androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC₅₀=4 μM) . CLP-3094 is a selective, potent GPR142** antagonist .

HY-16985S

Darolutamide-d4 ODM-201-d₄; BAY-1841788-d₄	Isotope-Labeled Compounds Androgen Receptor	Cancer
Darolutamide-d₄ (ODM-201-d₄) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive **androgen receptor (AR)** antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-136596

Apalutamide-COOH	Drug Metabolite	Cancer
Apalutamide-COOH is a metabolite of Apalutamide. Apalutamide is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-164552

ZNU-IMB-Z15	Apoptosis Androgen Receptor	Cancer
ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .

HY-16985R

Darolutamide (Standard) ODM-201 (Standard); BAY-1841788 (Standard)	Reference Standards Androgen Receptor	Cancer
Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive **androgen receptor (AR)** antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-16060S

Apalutamide-d4 ARN-509-d₄	Androgen Receptor	Cancer
Apalutamide-d₄ is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-152524

Androgen receptor antagonist 7	Androgen Receptor	Cancer
Androgen receptor antagonist 7 is an effective **androgen receptor** (AR) antagonist with an IC₅₀ value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI₅₀ value of 7.9 µM .

HY-121094

Androgen receptor allosteric antagonist 1	Estrogen Receptor/ERR	Cancer
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive **androgen receptor (AR)** antagonist with the K_i of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .

HY-130845

AR antagonist 1	Ligands for E3 Ligase Ligands for Target Protein for PROTAC	Cancer
AR antagonist 1 (compound 29) is a potent **androgen receptor (AR)** antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

HY-16060S1

Apalutamide-d3 ARN-509-d₃	Androgen Receptor	Cancer
Apalutamide-d₃ is the deuterium labeled Apalutamide . Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-14250

PF-998425	Androgen Receptor	Endocrinology
PF-998425 is a potent, selective nonsteroidal **androgen receptor (AR)** antagonist with an IC₅₀ of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research .

HY-111372A

(Rac)-Finerenone (Rac)-BAY 94-8862	Mineralocorticoid Receptor	Cardiovascular Disease
(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .

HY-125065

MK-4541	Androgen Receptor 5 alpha Reductase	Endocrinology Cancer
MK-4541 is an orally active and selective **androgen receptor** (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .

HY-111372S

Finerenone-d3 BAY 94-8862-d₃	Mineralocorticoid Receptor	Others
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal *mineralocorticoid receptor* (MR)** antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-111372S1

Finerenone-d5 1 Publications Verification BAY 94-8862-d₅	Isotope-Labeled Compounds Mineralocorticoid Receptor	Cardiovascular Disease
Finerenone-d₅ (BAY 94-8862-d₅) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal *mineralocorticoid receptor* (MR)** antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-B1866R

Linuron (Standard)	Reference Standards Androgen Receptor	Endocrinology
Linuron (Standard) is the analytical standard of Linuron. This product is intended for research and analytical applications. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .

HY-160692

AR antagonist 7	Androgen Receptor	Others
AR antagonist 7 (86) is an androgen receptor (AR) antagonist that can be used in the research of hair loss .

HY-144127

AR antagonist 3	Androgen Receptor	Cancer
AR antagonist 3 is a potent and selective **androgen receptor (AR)** antagonist with an IC₅₀ of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC₅₀= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .

HY-174391

AR antagonist 15	Androgen Receptor Apoptosis	Cancer
AR antagonist 15 is an orally active **androgen receptor (AR)** antagonist with the IC₅₀ of 97 nM for AR^T787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer.

HY-N9917

Galloylalbiflorin 6′-O-Galloylalbiflorin	Androgen Receptor	Endocrinology Cancer
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an **androgen receptor** (AR) antagonist (IC₅₀=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity .

HY-16060R

Apalutamide (Standard) ARN-509 (Standard)	Reference Standards Androgen Receptor	Cancer
Apalutamide (Standard) is the analytical standard of Apalutamide. This product is intended for research and analytical applications. Apalutamide (ARN-509) is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-16060S3

Apalutamide-d7 ARN-509-d₇	Androgen Receptor Isotope-Labeled Compounds	Cancer
Apalutamide-d₇ is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-119170

BMS-779333	Androgen Receptor	Neurological Disease Cancer
BMS-779333 is an orally active androgen receptor (AR) antagonist. BMS-779333 is promising for research of prostate cancer and seizure .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-15758

3,3'-Diindolylmethane 10+ Cited Publications DIM; Arundine; HB 236	Alkaloids other families Classification of Application Fields Plants Disease Research Fields Alkaloid Dimers Source Classification Cancer	Androgen Receptor Autophagy
3,3'-Diindolylmethane is a strong, pure **androgen receptor** (AR) antagonist.

HY-N2908

Atraric acid Methyl atrarate	Structural Classification Microorganisms Classification of Application Fields Phenols Essence, Fragrance Cosmetic Research Plants Inflammation/Immunology Disease Research Fields Cancer	Environmental Pollutants NF-κB Androgen Receptor p38 MAPK NO Synthase
Atraric acid (Methyl atrarate) is a specific **androgen receptor (AR)** antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .

HY-N0475

Triptophenolide Hypolide; (+)-Triptophenolide	Structural Classification Monophenols Classification of Application Fields Terpenoids Celastraceae Other Diseases Phenols Diterpenoids Tripterygium wilfordii Hook. f. Plants Disease Research Fields Source Classification	Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis
Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC₅₀ of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .

HY-15758R

3,3'-Diindolylmethane (Standard) DIM (Standard); Arundine (Standard); HB 236 (Standard)	Alkaloids Structural Classification other families Plants Alkaloid Dimers Source Classification	Reference Standards Androgen Receptor Autophagy
3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.

HY-N9917

Galloylalbiflorin 6′-O-Galloylalbiflorin	Paeonia lactiflora Pall. Polyphenols Plants Paeoniaceae Source Classification	Androgen Receptor
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an **androgen receptor** (AR) antagonist (IC₅₀=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity .

HY-W087006

p-Hydroxyphenylacetone	Structural Classification Other Monoterpenes Terpenoids Sargentodoxa cuneata (Oliv.) Rehd. et Wils. Plants Sargentodoxaceae Source Classification	Androgen Receptor
p-Hydroxyphenylacetone, a Raspberry ketone (HY-N1426) derivative, is an androgen receptor (AR) antagonist with an IC₅₀ of 420 μM in MDA-kb2 human breast cancer cells. p-Hydroxyphenylacetone can be used for breast cancer research .

HY-N0475R

Triptophenolide (Standard) Hypolide (Standard); (+)-Triptophenolide (Standard)	Structural Classification Monophenols Terpenoids Celastraceae Phenols Diterpenoids Tripterygium wilfordii Hook. f. Plants Source Classification	Reference Standards Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis
Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC₅₀ of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .

HY-N2908R

Atraric acid (Standard) Methyl atrarate (Standard)	Microorganisms Phenols Plants	Reference Standards Androgen Receptor NO Synthase p38 MAPK NF-κB
Atraric acid (Standard) is the analytical standard of Atraric acid. This product is intended for research and analytical applications. Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2].

Cat. No.	Product Name	Chemical Structure

HY-70002S1

Enzalutamide-d6
Enzalutamide-d₆ (MDV3100-d₆) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells .

HY-70002S

Deutenzalutamide
Deutenzalutamide (Enzalutamide-d₃) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .

HY-16985S

Darolutamide-d4

Darolutamide-d₄ (ODM-201-d₄) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-16060S

Apalutamide-d4
Apalutamide-d₄ is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-B1866S

Linuron-d6

Linuron-d₆ is the deuterium labeled Linuron (HY-B1866). Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .

HY-16060S1

Apalutamide-d3
Apalutamide-d₃ is the deuterium labeled Apalutamide . Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-111372S

Finerenone-d3

Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-111372S1

Finerenone-d5

1 Publications Verification

Finerenone-d₅ (BAY 94-8862-d₅) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-16060S3

Apalutamide-d7
Apalutamide-d₇ is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-16060S2

Apalutamide-13C,d3
Apalutamide- ¹³C,d₃ is the ¹³C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-14249S

Bicalutamide-d4
Bicalutamide-d₄ is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .

HY-14249S1

(R)-Bicalutamide-d5
(R)-Bicalutamide-d₅ is deuterated labeled (R)-Bicalutamide (HY-108250). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .

HY-W716464

Prochloraz-d7
Prochloraz-d₇ (BTS 40542-d₇) is the deuterium labeled Prochloraz (HY-B0845). Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC₅₀ values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC₅₀ of 1 μM .

HY-19337S1

Ketodarolutamide-d6

Ketodarolutamide-d₆ (BAY 1896953-d₆) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀ value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .

HY-19337S

Ketodarolutamide-d3

Ketodarolutamide-d₃ (BAY 1896953-d₃) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀ value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .

HY-W950003

(Rac)-Finerenone-d5

(Rac)-Finerenone-d₅ ((Rac)-BAY 94-8862-d₅) is the deuterium labeled (Rac)-Finerenone (HY-111372A). (Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

Cat. No.	Product Name		Classification

HY-114402

ARD-69		PROTAC Synthesis
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

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