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Results for "

Androgen receptor inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (91) 3β-HSD (1) 5 alpha Reductase (5) Adrenergic Receptor (1) Akt (1) Aldose Reductase (1) Apoptosis (26) Aryl Hydrocarbon Receptor (3) Autophagy (1) AUTOTACs (1) Bacterial (3) Calcium Channel (1) Cannabinoid Receptor (1) Caspase (1) CXCR (1) Cytochrome P450 (3) Drug Metabolite (1) Endogenous Metabolite (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (10) Fatty Acid Synthase (FASN) (1) Fungal (6) Glucocorticoid Receptor (2) Histone Acetyltransferase (4) Histone Methyltransferase (2) HSV (1) Insulin Receptor (1) Isotope-Labeled Compounds (5) LDLR (1) mAChR (1) Mineralocorticoid Receptor (1) MNK (1) Molecular Glues (1) NADPH Oxidase (1) NF-κB (3) NO Synthase (2) p38 MAPK (2) Parasite (3) Phosphodiesterase (PDE) (1) PPAR (2) Progesterone Receptor (2) Prostaglandin Receptor (1) PROTACs (9) PTHR (1) Reactive Oxygen Species (ROS) (1) Reference Standards (13) Src (2) Toll-like Receptor (TLR) (2) Topoisomerase (3)
By Research Areas:	Cancer (93) Cardiovascular Disease (2) Endocrinology (15) Infection (12) Inflammation/Immunology (7) Metabolic Disease (4) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (1)
Oligonucleotides:	Cholesterol (1)

111

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-158102

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

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

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) .

HY-173640

ID11916	Androgen Receptor Phosphodiesterase (PDE)	Cancer
ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .

HY-131953

Androgen receptor-IN-3	Androgen Receptor	Cancer
Androgen receptor-IN-3 (Compound 22) is an **androgen receptor** inhibitor. Androgen receptor-IN-3 inhibits AR-driven transcriptional activity in LNCaP cells, with an IC₅₀ of 5.04 μM .

HY-153772

Androgen receptor antagonist 8	Androgen Receptor	Cancer
Androgen receptor antagonist 8 (Example 13) is an **androgen receptor** antagonist. Androgen receptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC₅₀: 88 nM). Androgen receptor antagonist 8 can be used for prostate cancer research .

HY-151220

Androgen receptor-IN-4	Androgen Receptor	Others
Androgen receptor-IN-4 (Compound 206) is an **androgen receptor** inhibitor, and can be used for research of Kennedy's disease .

HY-169349

Androgen receptor antagonist 12	Androgen Receptor	Cancer
Androgen receptor antagonist 12 (Compound EF2) is an orally active **Androgen receptor** (AR) antagonist (IC₅₀: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .

HY-153276

Androgen receptor-IN-5	Androgen Receptor	Cancer
Androgen receptor-IN-5 is an **androgen receptor** inhibitor with potent anticancer effects. Androgen receptor-IN-5 also inhibits the production of IL-17A, IL- 17F and INF-γ (WO2023281097A1,Example 1/1) .

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-139623

A4B17	Androgen Receptor	Cancer
A4B17 is an **androgen receptor** N-terminal inhibitor for researching androgen-responsive 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-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-105122

Zanoterone WIN 49596	Androgen Receptor	Endocrinology Cancer
Zanoterone is an orally active antagonist of the androgen receptor (AR) with a K_i of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .

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-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-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-143535

HG122	Androgen Receptor	Cancer
HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant 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-164371

(+)-JJ-74-138	Androgen Receptor	Cancer
(+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .

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-123308

VPC13163	Androgen Receptor	Cancer
VPC13163 is a potent androgen receptor (AR) BF3 inhibitor with an IC₅₀ of 0.31 µM. VPC13163 has anticancer effects .

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-N0790

Lupeol 3 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-142923

AR antagonist 2	Androgen Receptor	Cancer
AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC₅₀ of 0.95 μM. AR antagonist 2 has the potential for cancer research .

HY-N2345

Procyanidin B3	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-172612

AR antagonist 13	Androgen Receptor	Cancer
AR antagonist 13 (compound 19) is an **androgen receptor** antagonist with inhibition rates exceeding 71.5% at 10 μM. AR antagonist 13 inhibits prostate cancer cell growth .

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-B0845

Prochloraz BTS 40542	Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon 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-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-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-W744741

Lupeol-d3	Isotope-Labeled Compounds Androgen Receptor Apoptosis	Cancer
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-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-114913

Fenarimol EL 222	Androgen Receptor Bacterial	Infection Endocrinology
Fenarimol (EL 222) is a potent and orally active fungicide. Fenarimol also is a **androgen receptor** inhibitor with an IC₅₀ value of 19 µM. Fenarimol decreases the mRNA expression of PBP C3, ODC, IGF-1 .

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-114246

ONC1-13B	Androgen Receptor	Cancer
ONC1-13B is a potent androgen receptor (AR) antagonist with the activity of effectively inhibiting PSA expression in prostate cancer cells. ONC1-13B can effectively inhibit PSA expression and prostate cancer cell proliferation under DHT stimulation. ONC1-13B exerts its anti-tumor effect by preventing androgen from binding to AR and its nuclear translocation .

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-N6714R

Alternariol (Standard)	Reference Standards Topoisomerase Androgen Receptor Estrogen Receptor/ERR Apoptosis	Infection Cancer
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-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-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-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-B0846

Dimethomorph	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-N2345R

Procyanidin B3 (Standard)	Reference Standards Histone Acetyltransferase Toll-like Receptor (TLR) Androgen Receptor	Inflammation/Immunology Cancer
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-403733B

(+)-JJ-450	Androgen Receptor Prostaglandin Receptor	Cancer
(+)-JJ-450 is a non-competitive antagonist targeting the **androgen receptor** (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003) .

HY-153918

(R)-SKBG-1	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-B0845R

Prochloraz (Standard) BTS 40542 (Standard)	Reference Standards Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon Receptor	Infection Endocrinology
Prochloraz (Standard) is the analytical standard of Prochloraz. This product is intended for research and analytical applications. 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 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-158101

BMS-986365 CC-94676	PROTACs Androgen Receptor	Cancer
BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, 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 significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697) .

Cat. No.	Product Name

HY-L126

Nuclear Receptor Compound Library

874 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 874 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-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.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-110028

Leelamine hydrochloride	Structural Classification other families Classification of Application Fields Pinaceae Terpenoids Source classification Diterpenoids Plants Disease Research Fields Pinus massoniana Lamb. Endocrinology	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-N0790

Lupeol 3 Publications Verification Clerodol; Monogynol B; Fagarasterol	Triterpenes Structural Classification other families Classification of Application Fields Terpenoids Source classification Plants Disease Research Fields 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-N2345

Procyanidin B3	Structural Classification Classification of Application Fields Source classification Plants Flavonoids other families Functional Molecules Research of Health Products Phenols Polyphenols Biflavones Disease Research Fields 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-N6714

Alternariol	Infection Structural Classification Microorganisms Classification of Application Fields Source classification Phenols Polyphenols Disease Research Fields	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-N1943

Ailanthone Δ13-Dehydrochaparrinone	Structural Classification Simaroubaceae Ailanthus altissima (Mill.) Swingle Classification of Application Fields Terpenoids Source classification Diterpenoids Plants Inflammation/Immunology Disease Research Fields	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-N7043

Isosilybin A 2 Publications Verification	Structural Classification Classification of Application Fields Source classification Cyamopsis tetragonoloba (L.) Taub. Plants Compositae Flavanonols Flavonoids Glycine soya Phenols Polyphenols Disease Research Fields Cancer	Apoptosis
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting *Akt-NF-κB-androgen* receptor (AR)** axis .

HY-N0790R

Lupeol (Standard) Clerodol (Standard); Monogynol B (Standard); Fagarasterol (Standard)	Triterpenes Structural Classification other families Terpenoids Source classification Plants	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 Source classification Phenols Polyphenols	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 Source classification Phenols Polyphenols Plants Biflavones	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-N7043R

Isosilybin A (Standard)	Flavanonols Structural Classification Flavonoids Glycine soya Source classification Phenols Polyphenols Cyamopsis tetragonoloba (L.) Taub. Plants Compositae	Reference Standards Apoptosis
Isosilybin A (Standard) is the analytical standard of Isosilybin A. This product is intended for research and analytical applications. Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .

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	Androgen Receptor NO Synthase p38 MAPK NF-κB
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-113289

Brassicasterol	Infection Animals Classification of Application Fields Source classification Disease Research Fields Steroids 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-N1486R

Ursonic acid (Standard) 3-Ketoursolic acid (Standard)	Triterpenes Structural Classification Ziziphus jujuba Terpenoids Source classification Plants Endogenous metabolite Rhamnaceae	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)	Structural Classification Microorganisms Phenols Plants	Reference Standards Androgen Receptor NO Synthase p38 MAPK NF-κB
Atraric acid (Standard) is the analytical standard of Atraric acid. This product is intended for research and analytical applications. Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2].

Cat. No.	Product Name	Chemical Structure

HY-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-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-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-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 .

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 the treatment 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