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Results for "

Androgen receptor inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (146) 11β-HSD (1) 3β-HSD (1) 5 alpha Reductase (6) Adenosine Receptor (1) Adrenergic Receptor (2) Akt (6) Aldose Reductase (1) Aminopeptidase (2) Amyloid-β (1) Antibiotic (1) Apoptosis (38) Aryl Hydrocarbon Receptor (3) Autophagy (3) AUTOTACs (1) Bacterial (4) Bcl-2 Family (4) c-Myc (4) Calcium Channel (2) Cannabinoid Receptor (1) Caspase (4) CDK (1) CXCR (1) Cytochrome P450 (5) Drug Metabolite (3) Endogenous Metabolite (2) Enteropeptidase (2) Environmental Pollutants (4) Epigenetic Reader Domain (3) ERK (4) Estrogen Receptor/ERR (12) Fatty Acid Synthase (FASN) (1) Ferroptosis (1) Fungal (8) GABA Receptor (1) Gap Junction Protein (2) Glucocorticoid Receptor (4) GSK-3 (2) HDAC (1) Herbicide (1) Histone Acetyltransferase (5) Histone Methyltransferase (5) HSP (2) HSV (1) Insulin Receptor (1) Integrin (2) Interleukin Related (1) Isotope-Labeled Compounds (11) JNK (1) Kallikrein (1) Keap1-Nrf2 (1) LDLR (1) Ligands for Target Protein for PROTAC (2) mAChR (1) Mineralocorticoid Receptor (2) Mitophagy (1) MMP (1) MNK (5) Molecular Glues (5) mTOR (4) NADPH Oxidase (1) NF-κB (4) NO Synthase (2) Opioid Receptor (2) Orphan Nuclear Receptor (2) p38 MAPK (2) Parasite (3) PARP (1) PDK-1 (1) Phosphodiesterase (PDE) (1) PI3K (4) PPAR (2) Progesterone Receptor (7) Prostaglandin Receptor (1) PROTACs (13) PTHR (1) Pyroptosis (2) Reactive Oxygen Species (ROS) (4) Reference Standards (18) ROR (1) Src (2) Tau Protein (1) TGF-β Receptor (1) Toll-like Receptor (TLR) (2) Topoisomerase (3) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (147) Cardiovascular Disease (3) Endocrinology (18) Infection (16) Inflammation/Immunology (14) Metabolic Disease (15) Neurological Disease (10)
Click Chemistry:	PROTAC Synthesis (1)
Oligonucleotides:	Cholesterol (1)

175

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-158101

BMS-986365 1 Publications Verification CC-94676	PROTACs Androgen Receptor	Cancer
BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC₅₀ of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .

HY-B0022

Flutamide Maximum Cited Publications 12 Publications Verification SCH 13521	Androgen Receptor	Cancer
Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome .

HY-13613

Dutasteride 3 Publications Verification GG 745; GI 198745	5 alpha Reductase Apoptosis	Cancer
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

HY-N0790

Lupeol 5 Publications Verification Clerodol; Monogynol B; Fagarasterol	Androgen Receptor Apoptosis	Cancer
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-158102

Rinzimetostat 1 Publications Verification ORIC-944	Histone Methyltransferase	Cancer
Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

HY-N1943

Ailanthone 2 Publications Verification Δ13-Dehydrochaparrinone	Androgen Receptor	Inflammation/Immunology Cancer
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC₅₀=69 nM) and constitutively active truncated AR splice variants (AR_1-651 IC₅₀=309 nM).

HY-136582

Masofaniten Androgen receptor-IN-2	Androgen Receptor	Cancer
Masofaniten (Androgen receptor-IN-2) is a potent and orally active **androgen receptor** inhibitor. Masofaniten has antitumor activity against prostate cancer .

HY-N2345

Procyanidin B3 1 Publications Verification	Histone Acetyltransferase Toll-like Receptor (TLR) Androgen Receptor	Inflammation/Immunology Cancer
Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen *receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting* the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .

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-B0111

Drospirenone 1 Publications Verification Dihydrospirorenone	Progesterone Receptor Androgen Receptor	Endocrinology Cancer
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and **androgen receptor** (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .

HY-153918

(R)-SKBG-1 1 Publications Verification	Androgen Receptor	Cancer
(R)-SKBG-1 is a covalent inhibitor targeting the RNA binding protein NONO. (R)-SKBG-1 can reduce the expression of androgen receptor (AR) and its splice variants, inhibiting cancer cell proliferation. (R)-SKBG-1 inhibits androgen receptor expression with IC₅₀ of 3.1 μM and 5.5 μM for AR-FL mRNA and AR-V7 mRNA, respectively. (R)-SKBG-1 interferes with the gene regulatory network of cancer cells and inhibits cancer cell growth by stabilizing the interaction between NONO and mRNA. (R)-SKBG-1 can be used in the study of cancers related to NONO dysfunction, such as prostate cancer .

HY-15103

AH3960	PTHR Androgen Receptor	Cancer
AH3960 (compound 16c) is an antagonist of **androgen receptor. AH3960 binds wild as well as T877** mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC₅₀ value of 0.82 μM. AH3960 also serves as an agonist of *parathyroid hormone receptor-1 (PTHR1)* .

HY-B1095

Chlormadinone acetate 1 Publications Verification	Progesterone Receptor Androgen Receptor Glucocorticoid Receptor GABA Receptor	Neurological Disease Metabolic Disease
Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABA_A receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .

HY-16079

AZD3514 3 Publications Verification	Androgen Receptor	Cancer
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC₅₀ value of 5.75. AZD3514 can be used for the research of prostate cancer .

HY-N6714

Alternariol	Topoisomerase Androgen Receptor Estrogen Receptor/ERR Apoptosis	Infection Cancer
Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen *Receptor) effects. Alternariol can induce apoptosis*, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

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-B0846

Dimethomorph	Environmental Pollutants Fungal Androgen Receptor Parasite	Infection
Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC₂₀ of 0.263 µM .

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-123875A

Ralaniten triacetate EPI-506	Androgen Receptor	Cancer
Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .

HY-149433

BWA-522	PROTACs Androgen Receptor Apoptosis	Cancer
BWA-522 is an orally active PROTAC degrader targeting full-length **androgen receptor (AR-FL*) and androgen* receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .

HY-110028

Leelamine hydrochloride	Cannabinoid Receptor Fatty Acid Synthase (FASN) Androgen Receptor	Endocrinology Cancer
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. Leelamine hydrochloride suppresses transcriptional activity of **androgen receptor**, which is known to regulate fatty acid synthesis ^[2,3].

HY-160020

ET516	Androgen Receptor	Cancer
ET516 is a potent inhibitor of **Androgen Receptor*. ET516 significantly inhibits* the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .

HY-156111

ARD-1676 1 Publications Verification	PROTACs Androgen Receptor	Cancer
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .

HY-109619

D4-abiraterone Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite	Androgen Receptor Cytochrome P450	Cancer
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**.

HY-132292

ARD-2128	PROTACs Androgen Receptor	Cancer
ARD-2128 is a highly potent, orally bioavailable *PROTAC androgen* receptor (AR)** degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .

HY-124292

Honokiol DCA 1 Publications Verification Honokiol dichloroacetate	Androgen Receptor	Cancer
Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level .

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-N15686

Torulene Torulin	Apoptosis Androgen Receptor Bcl-2 Family MMP	Cancer
Torulene (Torulin) is an orally active carotenoid with anti-cancer activity. Torulene inhibits proliferation and induces apoptosis of tumor cells via a mitochondrial signal pathway and the down-regulation of androgen receptor (AR) expression. Torulene can be used for the study of prostate cancer .

HY-164373

SC428	Androgen Receptor Apoptosis	Cancer
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .

HY-158102A

Rinzimetostat TFA 1 Publications Verification ORIC-944 TFA	Histone Methyltransferase	Cancer
Rinzimetostat (ORIC-944) TFA is the TFA salt form of ORIC (HY-158102). Rinzimetostat TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer .

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-155478

Androgen receptor-IN-6	Androgen Receptor	Cancer
Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC₅₀=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .

HY-103245

Cl-4AS-1	Androgen Receptor	Cancer
Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC₅₀ = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively) .

HY-163340

GA32	Glucocorticoid Receptor Androgen Receptor	Cancer
GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC₅₀ values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .

HY-156530

CYP11A1-IN-1	Cytochrome P450	Endocrinology
CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1, with IC₅₀ value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer .

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-139623

A4B17	Androgen Receptor	Cancer
A4B17 is an **androgen receptor** N-terminal inhibitor for researching androgen-responsive prostate cancer.

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-B2058

Triticonazole	Fungal Androgen Receptor	Infection
Triticonazole is an orally active triazole fungicide and androgen receptor antagonist. Triticonazole inhibits testosterone-induced androgen receptor activation and reduces basal testosterone secretion. Prenatal exposure to Triticonazole causes shortened anogenital distance in male rat fetuses and induces organ-specific histopathological changes in pigs. Triticonazole can be used for detoxification of seeds contaminated with fungal pathogens, but there is a risk of animal poisoning if the treated seeds are used as animal feed .

HY-P11007

β-catenin inhibitory peptoid	β-catenin Wnt Androgen Receptor	Cancer
β-catenin inhibitory peptoid (compound 13) inhibits the β-catenin:TCF interaction with an IC₅₀ of 5.44 µM. β-catenin inhibitory peptoid inhibits both Wnt (IC₅₀ of 0.105 µM) and androgen receptor (AR)-signaling (IC₅₀ of 1.02 µM) in prostate cancer cell lines. β-catenin inhibitory peptoid markedly diminishes cell proliferation of prostate cancer cell lines .

HY-111421

ODM-204	Androgen Receptor Cytochrome P450	Cancer
ODM-204 is novel nonsteroidal dual inhibitor of both **androgen receptor and CYP17A1 enzyme, with IC₅₀**s of 80 nM and 22 nM, respectively.

HY-106614

Osaterone acetate	Androgen Receptor 5 alpha Reductase	Endocrinology
Osaterone acetate is an orally active steroid anti-androgen agent, mainly used for benign prostatic hyperplasia (BPH) in dogs. Osaterone acetate competitively antagonizes **androgen receptor** and inhibits 5α-reductase, reducing the concentration of dihydrotestosterone (DHT) while blocking the growth-stimulating effects of testosterone and DHT on prostate cells. Osaterone acetate can rapidly alleviate the symptoms of BPH in dogs without affecting the fertility of breeding dogs .

HY-N0790R

Lupeol (Standard) Clerodol (Standard); Monogynol B (Standard); Fagarasterol (Standard)	Reference Standards Androgen Receptor Apoptosis	Cancer
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-W653896

Alternariol-d2	Isotope-Labeled Compounds Androgen Receptor Apoptosis Topoisomerase Estrogen Receptor/ERR	Infection
Alternariol-d₂ is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen *Receptor) effects. Alternariol can induce apoptosis*, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

HY-123163

JNJ-1250132 RWJ-66826; RTI-6617-003	Progesterone Receptor Glucocorticoid Receptor Androgen Receptor Estrogen Receptor/ERR	Endocrinology Cancer
JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC₅₀ of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC₅₀=0.50 nM) and the rat androgen receptor (AR) (IC₅₀=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC₅₀ >3000 nM) .

HY-13613R

Dutasteride (Standard) GG 745 (Standard); GI 198745 (Standard)	Reference Standards 5 alpha Reductase Apoptosis	Cancer
Dutasteride (Standard) is the analytical standard of Dutasteride. This product is intended for research and analytical applications. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

HY-174908

SJL2-1	Histone Methyltransferase 11β-HSD Androgen Receptor	Cancer
SJL2-1 is a PRMT5 inhibitor, with an IC₅₀ of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC) .

HY-118409

VPC-3033	Androgen Receptor	Endocrinology Cancer
VPC-3033 is an **androgen receptor** antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC₅₀: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC₅₀=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002) .

Cat. No.	Product Name

HY-L126

Nuclear Receptor Compound Library

1,040 compounds

Nuclear receptors (NR) are proteins found in cells that sense androgen and thyroid hormones and certain other molecules. They are ligand-activated transcription factors that participate in many aspects of human physiology and pathology, and regulate the expression of various important genes.

Nuclear receptors have become one of the main targets in the development of new drug strategies, providing a unique type of receptors for studying a variety of human diseases, such as breast cancers, skin disorders and diabetes. 13% of U.S. Food and Drug Administration (FDA) approved drugs target nuclear receptors.

MCE supplies a unique collection of 1,040 nuclear receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on nuclear receptor. MCE Nuclear Receptor Library is a useful tool for drugs research related to cancer, skin disease and diabetes.

Cat. No.	Product Name	Target	Research Area

HY-P11007

β-catenin inhibitory peptoid	β-catenin Wnt Androgen Receptor	Cancer
β-catenin inhibitory peptoid (compound 13) inhibits the β-catenin:TCF interaction with an IC₅₀ of 5.44 µM. β-catenin inhibitory peptoid inhibits both Wnt (IC₅₀ of 0.105 µM) and androgen receptor (AR)-signaling (IC₅₀ of 1.02 µM) in prostate cancer cell lines. β-catenin inhibitory peptoid markedly diminishes cell proliferation of prostate cancer cell lines .

HY-P11642A

Sialorphin TFA	Enteropeptidase Aminopeptidase Opioid Receptor ERK mTOR Androgen Receptor	Inflammation/Immunology
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .

HY-P2413

Ac-PPPHPHARIK-NH2	Androgen Receptor Src	Others
Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.

HY-P11642

Sialorphin	ERK Androgen Receptor Opioid Receptor Enteropeptidase mTOR Aminopeptidase	Neurological Disease Inflammation/Immunology Cancer
Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0790

Lupeol 5 Publications Verification Clerodol; Monogynol B; Fagarasterol	Triterpenes other families Classification of Application Fields Terpenoids Plants Disease Research Fields Source Classification Cancer	Androgen Receptor Apoptosis
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-N1943

Ailanthone 2 Publications Verification Δ13-Dehydrochaparrinone	Simaroubaceae Ailanthus altissima (Mill.) Swingle Classification of Application Fields Terpenoids Diterpenoids Plants Inflammation/Immunology Disease Research Fields Source Classification	Androgen Receptor
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC₅₀=69 nM) and constitutively active truncated AR splice variants (AR_1-651 IC₅₀=309 nM).

HY-113289

Brassicasterol 1 Publications Verification	Infection Animals Classification of Application Fields Disease Research Fields Steroids Source Classification Cancer	Akt Androgen Receptor Bacterial Drug Metabolite HSV
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC₅₀=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .

HY-N2345

Procyanidin B3 1 Publications Verification	Flavonoids other families Functional Molecules Classification of Application Fields Research of Health Products Phenols Polyphenols Plants Biflavones Disease Research Fields Source Classification Cancer	Histone Acetyltransferase Toll-like Receptor (TLR) Androgen Receptor
Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen *receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting* the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .

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-N6714

Alternariol	Infection Microorganisms Classification of Application Fields Phenols Polyphenols Disease Research Fields Source Classification	Topoisomerase Androgen Receptor Estrogen Receptor/ERR Apoptosis
Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen *Receptor) effects. Alternariol can induce apoptosis*, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

HY-110028

Leelamine hydrochloride	other families Classification of Application Fields Pinaceae Terpenoids Diterpenoids Plants Disease Research Fields Pinus massoniana Lamb. Endocrinology Source Classification	Cannabinoid Receptor Fatty Acid Synthase (FASN) Androgen Receptor
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. Leelamine hydrochloride suppresses transcriptional activity of **androgen receptor**, which is known to regulate fatty acid synthesis ^[2,3].

HY-N5124

Meloside A 4 Publications Verification Isovitexin 2''-O-glucoside; Isovitexin 2''-O-β-D-glucoside	Infection Structural Classification Flavonoids Classification of Application Fields Flavones Phenols Polyphenols Actaea dahurica Turcz. ex Fisch. & C. A. Mey. Plants Rhamnaceae Disease Research Fields Source Classification	Androgen Receptor Apoptosis Reactive Oxygen Species (ROS) Interleukin Related TGF-β Receptor
Meloside A (Isovitexin 2''-O-glucoside) is a flavonoid with antioxidant activity. Meloside A can inhibit cell apoptosis and ROS production. Meloside A can inhibit **androgen receptor** (AR) nuclear translocation and AR protein expression. Meloside A can reduce IL-6, TGF-β1 and DKK-1 levels. Meloside A can be used for the researches of inflammation and endocrinology, such as hair loss .

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-N15686

Torulene Torulin	Natural Products Microorganisms Source Classification	Apoptosis Androgen Receptor Bcl-2 Family MMP
Torulene (Torulin) is an orally active carotenoid with anti-cancer activity. Torulene inhibits proliferation and induces apoptosis of tumor cells via a mitochondrial signal pathway and the down-regulation of androgen receptor (AR) expression. Torulene can be used for the study of prostate cancer .

HY-135319

Strictinin	Structural Classification Phenols Polyphenols Camellia sinensis (L.) O. Ktze. Plants Source Classification Theaceae	Bacterial Antibiotic ERK JNK NF-κB ROR Apoptosis Caspase GSK-3 Akt PI3K
Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .

HY-N0790R

Lupeol (Standard) Clerodol (Standard); Monogynol B (Standard); Fagarasterol (Standard)	Triterpenes Structural Classification other families Terpenoids Plants Source Classification	Reference Standards Androgen Receptor Apoptosis
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-N6714R

Alternariol (Standard)	Structural Classification Microorganisms Phenols Polyphenols Source Classification	Reference Standards Topoisomerase Androgen Receptor Estrogen Receptor/ERR Apoptosis
Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

HY-N2345R

Procyanidin B3 (Standard)	Structural Classification Flavonoids other families Phenols Polyphenols Plants Biflavones Source Classification	Reference Standards Histone Acetyltransferase Toll-like Receptor (TLR) Androgen Receptor
Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .

HY-N1486R

Ursonic acid (Standard) 3-Ketoursolic acid (Standard)	Triterpenes Structural Classification Terpenoids Plants Actaea simplex (DC.) Wormsk. ex Fisch. & C. A. Mey. Endogenous metabolite Rhamnaceae Source Classification	Reference Standards Apoptosis Endogenous Metabolite NF-κB
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model

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].

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 .

Cat. No.	Product Name	Chemical Structure

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-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-W653896

Alternariol-d2

Alternariol-d₂ is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

HY-B0561S4

Spironolactone-d6-1

Spironolactone-d₆-1 is the deuterium labeled Spironolactone (HY-B0561). Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC₅₀=24 nM) and androgen receptor (IC₅₀=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca ²⁺ channels to exert antihypertensive effects .

HY-W744741

Lupeol-d3
Lupeol-d₃ is the deuterium labeled Lupeol (HY-N0790). Lupeol is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor?(AR)?inhibitor and can be used for?cancer?research, especially prostate?cancer?of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-13613S

Dutasteride-13C6
Dutasteride- ¹³C₆ is the ¹³C labeled Dutasteride . Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

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-B0846S

Dimethomorph-d8
Dimethomorph-d₈ is the deuterium labeled Dimethomorph . Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM .

HY-B1095S1

Chlormadinone acetate-d6-1

Chlormadinone acetate-d₆-1 is deuterium labeled Chlormadinone acetate (HY-B1095). Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABA_A receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .

HY-B1095S2

Chlormadinone acetate-d3

Chlormadinone acetate-d₃ is the deuterium labeled Chlormadinone acetate (HY-B1095). Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABA_A receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .

HY-13613S2

Dutasteride-13C,15N,d
Dutasteride- ¹³C, ¹⁵N,d is ¹⁵N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

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 .

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).

Cat. No.	Product Name		Classification