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Results for "

androgen receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (328) 11β-HSD (1) 3β-HSD (1) 5 alpha Reductase (6) Adenosine Receptor (2) Adrenergic Receptor (4) Akt (12) Aldose Reductase (2) Aminopeptidase (2) Amyloid-β (1) Antibiotic (1) Apoptosis (53) Aryl Hydrocarbon Receptor (3) AUTACs (1) Autophagy (22) AUTOTACs (4) Bacterial (7) Bcl-2 Family (5) c-Myc (4) Calcium Channel (4) Cannabinoid Receptor (1) Caspase (11) CDK (3) CFTR (3) CXCR (1) Cytochrome P450 (9) Drug Derivative (4) Drug Isomer (2) Drug Metabolite (11) E1/E2/E3 Enzyme (3) E3 Ligase Ligand-Linker Conjugates (3) Endogenous Metabolite (8) Enteropeptidase (2) Environmental Pollutants (6) Epigenetic Reader Domain (6) ERK (4) Estrogen Receptor/ERR (23) Fatty Acid Synthase (FASN) (1) Ferroptosis (1) Fungal (8) GABA Receptor (1) Gap Junction Protein (2) Glucocorticoid Receptor (11) GLUT (1) GnRH Receptor (2) GSK-3 (2) HDAC (1) Herbicide (1) Histone Acetyltransferase (5) Histone Methyltransferase (8) HIV (4) HSP (2) HSV (1) Insulin Receptor (1) Integrin (2) Interleukin Related (1) Isotope-Labeled Compounds (35) JNK (3) Kallikrein (1) Keap1-Nrf2 (1) LDLR (1) Ligands for E3 Ligase (8) Ligands for Target Protein for PROTAC (16) mAChR (1) Mineralocorticoid Receptor (14) Mitochondrial Metabolism (1) Mitophagy (1) MMP (1) MNK (5) Molecular Glues (9) mTOR (7) NADPH Oxidase (1) Neprilysin (1) NF-κB (6) NO Synthase (2) Opioid Receptor (2) Orphan Nuclear Receptor (2) p38 MAPK (3) Parasite (7) PARP (3) PDK-1 (1) Phosphatase (1) Phosphodiesterase (PDE) (1) PI3K (9) PPAR (2) Progesterone Receptor (17) Prostaglandin Receptor (2) PROTAC Linkers (2) PROTACs (37) PSMA (2) PTHR (1) Pyroptosis (2) Reactive Oxygen Species (ROS) (5) Reference Standards (42) ROR (1) SNIPERs (2) SOD (1) Sodium Channel (2) Src (3) Tau Protein (1) TGF-β Receptor (1) Thyroid Hormone Receptor (3) Toll-like Receptor (TLR) (2) Topoisomerase (3) Wnt (2) Zinc Finger Protein (1) β-catenin (2)
By Research Areas:	Cancer (310) Cardiovascular Disease (20) Endocrinology (78) Infection (23) Inflammation/Immunology (24) Metabolic Disease (46) Neurological Disease (21)
Click Chemistry:	PROTAC Synthesis (3) Alkynes (3)
Oligonucleotides:	Cholesterol (1)

414

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-138641

Bavdegalutamide 5+ Cited Publications ARV-110	PROTACs Androgen Receptor	Cancer
Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986)) .

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-153342

Luxdegalutamide 2 Publications Verification ARV-766; JSB462	PROTACs Androgen Receptor	Cancer
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .

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-12111

BMS-564929 5+ Cited Publications	Androgen Receptor	Endocrinology
BMS-564929 is an **androgen receptor** (AR) agonist, binds to androgen receptor (AR) with a K_i of 2.11±0.16 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-122025

AC-262536 1 Publications Verification	Androgen Receptor	Metabolic Disease
AC-262536 is a selective and non-steroidal **androgen receptor modulators (SARMs*) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen* receptor, with an affinity in the low nanomolar range (1-10 nM) .

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-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-100348

EPI-001	Androgen Receptor PPAR Apoptosis	Cancer
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .

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-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-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-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-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-133045

VHL Ligand 8	Ligands for E3 Ligase	Cancer
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM .

HY-145709

Ar-V7-IN-1	Androgen Receptor	Cancer
Ar-V7-IN-1 is a potent inhibitor of Ar-V7. Ar-V7-IN-1 inhibits the transcriptional activity of androgen receptor (AR) and the secretion of prostate-specific antigen (PSA) with an eGFP IC₅₀ of 1232 nM and the PSA IC₅₀ of 1391 μM. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer .

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-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-170329

PROTAC AR Degrader-8	PROTACs Androgen Receptor Apoptosis	Cancer
PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC₅₀s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC₅₀ of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC₅₀ values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer .

HY-18102

GLPG0492 5+ Cited Publications	Androgen Receptor	Neurological Disease
GLPG0492 is an orally active, non-steroidal selective **androgen receptor** modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

HY-103246

TFM-4AS-1	Androgen Receptor	Cancer
TFM-4AS-1 is a *selective androgen* receptor modulator (SARM)*, and a potent androgen* receptor (AR) ligand with an IC₅₀ of 38 nM. TFM-4AS-1 is a gene-selective agonist .

HY-139436

ARD-2585	PROTACs Androgen Receptor	Cancer
ARD-2585 is an exceptionally potent and orally active PROTAC degrader of **androgen receptor** .

HY-149862

ARD-2051 1 Publications Verification	PROTACs Androgen Receptor	Cancer
ARD-2051 is a selective and orally active **androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC₅₀** values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .

HY-43962

Androgen receptor ligand 3	Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
Androgen receptor ligand 3 is an androgen receptor (AR) ligand. Androgen receptor ligand 3 is linked to an IAP ligand via a linker to form an ERα PROTAC degrader.

HY-13607

BMS-641988	Androgen Receptor	Cancer
BMS-641988 (compound 23) is an oral active nonsteroidal **androgen receptor antagonist with the K_i** of 1.7 nM. BMS-641988 shows anticancer activity .

HY-120018

VPC-13566	Androgen Receptor	Cancer
VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of 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-112689

Androgen receptor antagonist 9	Androgen Receptor	Endocrinology
Androgen receptor antagonist 9 (compound 28) is an antagonist of the androgen receptor .

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-164807

SARD279	PROTACs Androgen Receptor	Cancer
SARD279 is a potent and selective **Androgen Receptor degrader with DC₅₀** value of 1099 nM. SARD279 can be used in prostate cancer research .(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))

HY-171048

GTx-027	Androgen Receptor	Endocrinology Cancer
GTx-027 is an orally active and non-steroidal selective **androgen receptor** modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI) .

HY-N16483

Procyanidin B2-3'-O-gallate	Apoptosis Caspase Bcl-2 Family PARP Androgen Receptor	Cancer
Procyanidin B2-3'-O-gallate is a mono-gallate ester that can be found in grape seed extract. Procyanidin B2-3'-O-gallate induces cleavage of caspase-9, caspase-3, and PARP, reduces levels of Bcl-2, Bcl-Xl, and **androgen receptor and induces apoptosis**. Procyanidin B2-3'-O-gallate can be used for the research of prostate cancer .

HY-131388

ABM-14	Ligands for Target Protein for PROTAC	Cancer
ABM-14 is a ligand for targeting androgen receptor (AR) for PROTAC. ABM-14 binds to a ligand for VHL via linker to form ARCC-4 (HY-130492) to degrade AR .

HY-157491

K2-B4-5e	PROTACs Androgen Receptor Epigenetic Reader Domain	Cancer
K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells .

HY-163940

LX1	Aldose Reductase Androgen Receptor	Cancer
LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7 and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth .

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-133046

VHL Ligand-Linker Conjugates 17	E3 Ligase Ligand-Linker Conjugates	Cancer
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader . VHL Ligand-Linker Conjugates 17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-171809

AR ligand 42	Ligands for Target Protein for PROTAC Androgen Receptor	Endocrinology
AR ligand 42 is a **androgen receptor** ligand. AR ligand 42 can be used to synthesize androgen receptor PROTAC degrader ITRI-90 (HY-171808) .

HY-156751

(Rac)-GDC-2992 (Rac)-RO7656594; PROTAC AR Degrader-6	PROTACs Androgen Receptor	Cancer
(Rac)-GDC-2992 (Compound 1) is a PROTAC **androgen receptor** degrader (DC₅₀: 10 nM in VCaP cell). (Rac)-GDC-2992 blocks the process of androgen receptor transduction and also degrades the receptor itself. (Rac)-GDC-2992 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975) .

HY-177694

PROTAC AR Degrader-11	PROTACs Androgen Receptor	Cancer
PROTAC AR Degrader-11 is a potent **androgen receptor** and androgen receptor splice variant-7 PROTAC degrader. PROTAC AR Degrader-11 shows potent cytotoxicity against both CWR22RV1 cells and VCaP cells. PROTAC AR Degrader-11 can be used in prostate cancer research . (Structure Note: Pink: Androgen Receptor ligand (HY-171809); Blue: CRBN ligand (HY-A0003); Black: linker (HY-169966))

HY-103578

S-40503	Androgen Receptor	Cancer
S-40503 is an orally active and selective **androgen receptor** modulator. S-40503 significantly increases the bone mineral density (BMD) and biomechanical strength of femoral cortical bone .

HY-W653723

N-Nitrosodicyclohexylamine NDCHA	Androgen Receptor	Endocrinology
N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .

HY-174244

3βHSD1-IN-1	3β-HSD Androgen Receptor	Cancer
3βHSD1-IN-1 (Compound 46) is a 3β-hydroxysteroid dehydrogenase 1 (3βHSD1) inhibitor with an IC₅₀ of 55 nM. 3βHSD1-IN-1 can effectively inhibit **androgen receptor** activity. 3βHSD1-IN-1 can be used in the research of diseases such as prostate cancer .

HY-160221

PROTAC AR Degrader-7	PROTACs Androgen Receptor	Cancer
PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting **androgen receptor with an IC₅₀** value of 3 nM. PROTAC AR Degrader-7 is composed of PROTAC target protein ligand AR ligand-32 (HY-170303) (red part), E3 ligase ligand E3 ligase Ligand 44 (HY-170304) (blue part) and PROTAC Linker N-Boc-piperazine (HY-30105) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 145 (HY-170305) .

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-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.

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.

HY-L935

Molecular Glue POI binding Fragment library

1039 compounds

POI (Protein of Interest) refers to the target protein, namely the disease-causing protein or key functional protein that undergoes degradation or functional modulation in molecular glue-mediated processes. The Molecular Glue POI Library consists of a series of fragments that can specifically bind to different types of POIs. As key components of molecular glues, these ligands form stable interactions with target proteins, laying the foundation for molecular glues to induce the interaction between POIs and E3 ubiquitin ligases. The covered POIs include various types such as cancer-associated GSPT1, androgen receptors, and abnormally aggregated proteins linked to neurodegenerative diseases.

This fragment library can be applied to the screening and optimization of targeted protein degraders. By screening ligands with high affinity and strong selectivity for specific POIs from the library, core structures can be identified to develop novel molecular glues. For instance, optimization of ligands targeting GSPT1 has yielded molecular glue degraders with enhanced degradation activity. Since many POIs are difficult to drug due to the lack of traditional small-molecule binding pockets, some ligands in the POI Ligand Library can modulate such POIs by inducing protein-protein interactions, thereby further expanding the scope of drug discovery for undruggable targets.

MCE has compiled a POI Fragment Library comprising thousands of POI fragments with molecular weights ranging from 150 to 400. This compound library can be widely applied in Molecular Glue research and development.

Cat. No.	Product Name	Type

HY-W011927

4,4'-Sulfonyldiphenol

Bisphenol S; Bis(4-hydroxyphenyl) sulfone

Biochemical Assay Reagents

4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an oally ative estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC₅₀ values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae .

HY-W011927R

4,4'-Sulfonyldiphenol (Standard)

Bisphenol S (Standard); Bis(4-hydroxyphenyl) sulfone (Standard)

Biochemical Assay Reagents

4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC₅₀ values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.

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-P11443

SRC2-2 peptide	Androgen Receptor	Cancer
SRC2-2 peptide is a a coactivator-derived mimic targeting androgen receptor (AR) ligand. SRC2-2 peptide is promising for research of prostate cancer .

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-P2446

ORG 30276 APTAA-LHRH	GnRH Receptor	Endocrinology
ORG 30276 (APTAA-LHRH) is a potent GnRH antagonist that effectively reduces serum LH and FSH levels in male rats. ORG 30276 significantly decreases unoccupied pituitary GnRH receptors, leading to suppressed gonadotropin secretion. ORG 30276 treatment results in a considerable reduction in mRNA levels of gonadotropin beta-subunits in the pituitary gland. ORG 30276's effects on gonadotropin dynamics can be selectively reversed by the replacement of specific sex steroids, with androgens being particularly effective for the FSH beta-subunit mRNA levels.

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 .

HY-P11660

β-catenin-IN-10	β-catenin Wnt Androgen Receptor	Cancer
β-catenin-IN-10 is a β-catenin:TCF4 interaction inhibitor with an IC₅₀ of 5.44 μM. β-catenin-IN-10 inhibits the Wnt and AR signaling pathways with IC₅₀ values of 0.105 μM and 1.02 μM, respectively. β-catenin-IN-10 suppresses the proliferation of castration-resistant prostate cancer cells. β-catenin-IN-10 is applicable to research related to prostate cancer .

Cat. No.	Product Name	Target	Research Area	Image

HY-P992149

Lutropin alfa	GnRH Receptor	Endocrinology
Lutropin alfa is a recombinant human luteinizing hormone (LH). Lutropin alfa consists of non-covalently linked α and β subunits, and its activity is similar to that of natural luteinizing hormone. Lutropin alfa is used to stimulate follicular development in infertility .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-14650

DHEA Maximum Cited Publications 50 Publications Verification Prasterone; Dehydroisoandrosterone; Dehydroepiandrosterone	Structural Classification Human Gut Microbiota Metabolites Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification Cancer	Environmental Pollutants Endogenous Metabolite Androgen Receptor
DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.

HY-B0469

Medroxyprogesterone acetate 30+ Cited Publications Medroxyprogesterone 17-acetate; Farlutin	Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification Cancer	Progesterone Receptor Androgen Receptor Glucocorticoid Receptor Endogenous Metabolite
Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, *androgen* and glucocorticoid receptors .

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-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-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-N2026

Propylparaben 1 Publications Verification Propyl parahydroxybenzoate; Propyl 4-hydroxybenzoate	Infection Structural Classification Natural Products Monophenols Preservatives Classification of Application Fields Phenols Cosmetic Research Endogenous metabolite Disease Research Fields Source Classification Food Research	Bacterial Estrogen Receptor/ERR Sodium Channel PI3K JNK Akt Apoptosis
Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is an orally active weak estrogen receptor agonist. Propylparaben regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury .

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-15194

Dimethylcurcumin 10+ Cited Publications ASC-J9; GO-Y025	Zingiber officinale Roscoe Classification of Application Fields Simple Phenylpropanols Phenylpropanoids Plants Disease Research Fields Source Classification Zingiberaceae Cancer	Androgen Receptor
Dimethylcurcumin (ASC-J9) is an **androgen receptor** degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.

HY-N4089

Quercetin 3-gentiobioside	Flavonols Structural Classification Flavonoids other families Classification of Application Fields Phenols Polyphenols Metabolic Disease Plants Disease Research Fields Source Classification	Aldose Reductase Cytochrome P450
Quercetin 3-gentiobioside is a flavonoid found in Artemisia iwayomogi. Quercetin 3-gentiobioside inhibits aromatase with an K_i of 46.77 nM. Quercetin 3-gentiobioside inhibits aldose reductase (AR) and the formation of advanced glycation end products (AGEs), with IC₅₀ values of 10.60 μM and 109.46 μM, respectively. Quercetin 3-gentiobioside inhibits proliferation of cancer cells and fibroblast-like synoviocytes. Quercetin 3-gentiobioside can be used for the research of cancer, such as lung carcinoma .

HY-N3755

Dihydroresveratrol	Human Gut Microbiota Metabolites Classification of Application Fields Phenols Polyphenols Plants Endogenous metabolite Disease Research Fields Dioscorea bulbifera Linn. Dioscoreaceae Source Classification Cancer	Estrogen Receptor/ERR
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations .

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-N7045

Isosilybin B 2 Publications Verification	Flavanonols Flavonoids Glycine soya Classification of Application Fields Phenols Polyphenols Cyamopsis tetragonoloba (L.) Taub. Plants Compositae Disease Research Fields Source Classification Cancer	Androgen Receptor Apoptosis CDK Caspase PSMA
Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer .

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-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-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-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-B0469R

Medroxyprogesterone acetate (Standard) 30+ Cited Publications Medroxyprogesterone 17-acetate(Standard); Farlutin (Standard)	Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification Cancer	Reference Standards Progesterone Receptor Androgen Receptor Glucocorticoid Receptor Endogenous Metabolite
Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, *androgen* and glucocorticoid receptors .

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-N2026A

Propylparaben sodium 1 Publications Verification Propyl parahydroxybenzoate sodium; Propyl 4-hydroxybenzoate sodium	Infection Structural Classification Natural Products Classification of Application Fields Cosmetic Research Endogenous metabolite Disease Research Fields Source Classification	Estrogen Receptor/ERR Bacterial Sodium Channel PI3K JNK Akt Apoptosis
Propylparaben (Propyl parahydroxybenzoate) sodium is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben sodium is an orally active weak estrogen receptor agonist. Propylparaben sodium regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben sodium is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury .

HY-N16483

Procyanidin B2-3'-O-gallate	Structural Classification Vitis vinifera cv. Zalema Phenols Polyphenols Plants Vitaceae Source Classification	Apoptosis Caspase Bcl-2 Family PARP Androgen Receptor
Procyanidin B2-3'-O-gallate is a mono-gallate ester that can be found in grape seed extract. Procyanidin B2-3'-O-gallate induces cleavage of caspase-9, caspase-3, and PARP, reduces levels of Bcl-2, Bcl-Xl, and **androgen receptor and induces apoptosis**. Procyanidin B2-3'-O-gallate can be used for the research of prostate cancer .

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-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-15194R

Dimethylcurcumin (Standard) ASC-J9 (Standard); GO-Y025 (Standard)	Zingiber officinale Roscoe Structural Classification Simple Phenylpropanols Phenylpropanoids Plants Source Classification Zingiberaceae	Androgen Receptor Reference Standards
Dimethylcurcumin (Standard) is the analytical standard of Dimethylcurcumin. This product is intended for research and analytical applications. Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.

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-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-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-N7045R

Isosilybin B (Standard)	Flavanonols Structural Classification Flavonoids Glycine soya Phenols Polyphenols Cyamopsis tetragonoloba (L.) Taub. Plants Compositae Source Classification	Reference Standards Androgen Receptor Apoptosis CDK Caspase PSMA
Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer .

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-N13475

(3R,3′R)-Astaxanthin	Structural Classification Natural Products Microorganisms Source Classification	Androgen Receptor
(3R,3′R)-Astaxanthin is an **androgen receptor** binder. (3R,3′R)-Astaxanthin can be used in the research of prostate cancer .

HY-W585917

Bisphenol F bis(2-chloro-1-propanol) ether BFDGE·2HCl	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Androgen Receptor
Bisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) is an **androgen receptor antagonist with a human IC₅₀** of 18 μM. Bisphenol F bis(2-chloro-1-propanol) ether binds to the androgen receptor. Bisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) can be used for research on hormonal activity .

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-W011927S

4,4'-Sulfonyldiphenol-d8

1 Publications Verification

4,4'-Sulfonyldiphenol-d₈ (Bisphenol S (4,4'-Sulfonyldiphenol)-d₈) is the deuterium labeled 4,4'-Sulfonyldiphenol (HY-W011927).4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC₅₀ values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.

HY-135794S

11-Ketodihydrotestosterone-d3

11-Ketodihydrotestosterone-d₃ is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a K_i of 20.4 nM and an EC₅₀ of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer 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-B0469S

Medroxyprogesterone acetate-d3 1 Publications Verification
Medroxyprogesterone acetate-d₃ is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors .

HY-B0561S1

Spironolactone-d3
Spironolactone-d₃ is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes .

HY-141901S1

DHEA-d5

DHEA-d₅ (Prasterone-d₅; Dehydroisoandrosterone-d₅; Dehydroepiandrosterone-d₅) is the deuterium labeled DHEA (HY-14650). DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.

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-B1986S

p,p'-DDE-d8
p,p'-DDE-d₈ is the deuterium labeled p,p'-DDE . p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC₅₀ of 5 μM and a K_i of 3.5 μM .

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-W754151

N-Desmethyl apalutamide-d4

N-Desmethyl apalutamide-d₄ is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .

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-B0561S

Spironolactone-d7
Spironolactone-d₇ is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes .

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-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-B0251S

Eplerenone-d3
Eplerenone-d₃ is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC₅₀ of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch .

HY-13676S

Megestrol acetate-d3

Megestrol acetate-d₃ is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .

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-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-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-B0561S2

Spironolactone-d3-1
Spironolactone-d₃-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes .

HY-13604S

Cyproterone acetate-d3
Cyproterone acetate-d₃ is deuterium labeled Cyproterone acetate. Cyproterone acetate is an anti-androgen (IC₅₀=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors .

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-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-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-W753141

p,p'-DDE-13C12
p,p'-DDE- ¹³C₁₂ is ¹³C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent **androgen receptor antagonist, with an IC₅₀ of 5 μM and a K_i** of 3.5 μM .

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-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-13676S1

Megestrol acetate-d3-1

Megestrol acetate-d₃-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .

HY-106827S1

Trimegestone-13C,d3

Trimegestone- ¹³C,d₃ is ¹³C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC₅₀ value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC₅₀=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .

HY-135331S

N-Desmethyl-Apalutamide-15N,d4

N-Desmethyl-Apalutamide-15N,d4 is the ¹⁵N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .

HY-18102BS

GLPG0492-13C,d3 racemate

GLPG0492- ¹³C,d₃ racemate is ¹³C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

HY-13604S1

Cyproterone acetate-d6
Cyproterone acetate-d₆ is the deuterium labeled Cyproterone acetate (HY-13604). Cyproterone acetate is an *anti-androgen* (IC₅₀=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors .

HY-B0469S1

Medroxyprogesterone acetate-d7
Medroxyprogesterone acetate-d₇ (Medroxyprogesterone 17-acetate-d₇) is the deuterium labeled Medroxyprogesterone acetate (HY-B0469) . Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors .

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).

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-106203

Crinecerfont SSR-125543		Alkynes
Crinecerfont (SSR-125543) is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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).

HY-106203A

Crinecerfont hydrochloride SSR-125543 hydrochloride		Alkynes
Crinecerfont (SSR-125543) hydrochloride is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont hydrochloride blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont hydrochloride improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont hydrochloride can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency . Crinecerfont hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-139659

ARD-61		PROTAC Synthesis
ARD-61 is a highly potent, effective and specific *PROTAC androgen* receptor (AR)** degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-133020

ARD-266		PROTAC Synthesis
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based **Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀** values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-16247

Apoptone HE3235		Alkynes
Apoptone (HE3235) is an orally active 3β-androstanediol analog. Apoptone reduces the expression of androgen receptor (Androgen *receptor) and decreases intratumoral androgen* levels. Apoptone exhibits anticancer activity against castration-resistant prostate cancer .

Cat. No.	Product Name		Classification

HY-113289

Brassicasterol 1 Publications Verification		Cholesterol
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 .

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