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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

Results for "

AR LNCaP cell

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (1) Akt (1) Androgen Receptor (37) Apoptosis (5) Autophagy (3) AUTOTACs (1) Bacterial (1) Bcl-2 Family (1) Caspase (2) E1/E2/E3 Enzyme (1) Environmental Pollutants (1) Epigenetic Reader Domain (1) Histone Acetyltransferase (1) Isotope-Labeled Compounds (4) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (2) Molecular Glues (1) NF-κB (2) NO Synthase (2) p38 MAPK (2) PARP (1) PROTAC Linkers (1) PROTACs (9) Pyroptosis (1) Reactive Oxygen Species (ROS) (1) Reference Standards (3) Ser/Thr Protease (1)
By Research Areas:	Cancer (42) Endocrinology (2) Infection (1) Inflammation/Immunology (4)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

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Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Programmed Cell Death 4 (PDCD4) Itk TOPK NAMPT ALCAM/CD166 GDNF Receptor BCL6 Tim3 VISTA BMI1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-70002

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

HY-16985

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

HY-158113

CBPD-409	Histone Acetyltransferase PROTACs	Cancer
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC₅₀ of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC₅₀s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .

HY-N2908

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

HY-70002R

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

HY-130992

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

HY-70002S1

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

HY-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-19337

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

HY-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-70002S

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

HY-115282A

JNJ-63576253 1 Publications Verification TRC-253	Androgen Receptor	Cancer
JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC₅₀s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .

HY-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-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-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-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-133020

ARD-266	PROTACs Androgen Receptor	Cancer
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-162702

AZ'3137	PROTACs Androgen Receptor	Cancer
AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC₅₀ value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC₅₀ of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI₅₀ value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Pink: AR Ligand (HY-172954); Blue: CRBN ligand (HY-172955); Black: linker (HY-W262798); E3 Ligand+Linker: HY-172956) .

HY-175652

AZD9750	PROTACs Adenosine Receptor	Cancer
AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR ^L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .

HY-16985S

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

HY-163641

AR Degrader-1	Molecular Glues Androgen Receptor E1/E2/E3 Enzyme	Cancer
AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells .

HY-175455

LYA914	PROTACs Androgen Receptor Akt	Cancer
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .

HY-176128

BWA-6047	PROTACs Androgen Receptor Apoptosis PARP Caspase	Cancer
BWA-6047 is an oral active PROTAC degrader targeting *AR/AR-V7* and GSPT1 with DC₅₀ values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .

HY-16985R

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

HY-163510

AR/AR-V7-IN-1	Androgen Receptor	Cancer
AR/AR-V7-IN-1 (Compound 20i) is an *AR/ARV7* inhibitor (IC₅₀ = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC₅₀ values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .

HY-149914

WCA-814	Androgen Receptor	Cancer
WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC₅₀: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell) .

HY-124585

Y08060	Epigenetic Reader Domain	Cancer
Y08060 is a selective BET inhibitor. Y08060 inhibits the viability of C4-2B and LNCaP cell lines with IC₅₀ values of 3.23 and 4.41 μM. Y08060 can suppress colony formation as well as AR expression in prostate cancer cell line. Y08060 can be studied in prostate cancer research .

HY-133044

Boc-Pip-alkyne-Ph-COOH	PROTAC Linkers	Cancer
Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH 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-N8504

Neoaureothin NSC 260179; Spectinabilin	Bacterial	Infection
Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC₅₀=13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC₅₀=1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC₅₀s=34.3, 47, and 37.2 μg/mL, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50=0.84 μg/mL) and increases survival of P. densiflora trees inoculated with B. xylophilus.

HY-111231

CH4933468	Androgen Receptor	Cancer
CH4933468 is a thiohydantoin derivative, shows androgen receptor (AR) pure antagonist activity in vitro. CH4933468 inhibits AR-mediated transactivation and proliferation of LNCaP and LNCaP-BC2 cells. CH4933468 can be used for castration-resistant prostate cancer (CRPC) research .

HY-126464

Estromustine EoM	Androgen Receptor	Cancer
Estromustine (EoM) is the active metabolite of Estramustine phosphate (HY-13627A). Estromustine binds to mutant androgen receptor (m-AR) with EC₅₀ of 2.6 μM in LNCaP, exhibits cytotoxicity in human prostate cells LNCaP with IC₅₀ of 9.73 μM .

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-173409

AR antagonist 11	Androgen Receptor Ser/Thr Protease	Inflammation/Immunology
AR antagonist 11 (Compound c2) is a selective AR antagonist with an IC₅₀ of 0.019 μM. AR antagonist 11 is also effective against AR ^F877L/T878A mutant (IC₅₀: 1.03 μM). AR antagonist 11 inhibits LNCaP cell proliferation and reduces PSA protein expression (IC₅₀: 0.54 μM). AR antagonist 11 can be used for research of prostate cancer (PCa) .

HY-115282

JNJ-63576253 free base TRC-253 free base	Androgen Receptor	Cancer
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC₅₀s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .

HY-179050

Androgen receptor-IN-7	Androgen Receptor Reactive Oxygen Species (ROS)	Cancer
Androgen receptor-IN-7 is a potent androgen receptor (AR) inhibitor. Androgen receptor-IN-7 exhibits potent anticancer activity against PC-3 cells (IC₅₀ =370.37 nM) and LNCaP cells via both AR-dependent and AR-independent pathways. Androgen receptor-IN-7 induces ROS production in PC-3 cells. Androgen receptor-IN-7 can be used for prostate cancer research .

HY-178148

AR antagonist 17	Androgen Receptor	Endocrinology Cancer
AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC₅₀ = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .

HY-161741

VinclozolinM2-2204	AUTOTACs Androgen Receptor	Cancer
VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC₅₀ of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR ⁺LC3 ⁺ autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer .(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))

HY-118375

Phenylbutyl isoselenocyanate ISC-4	Apoptosis	Cancer
Phenylbutyl isoselenocyanate (ISC-4) is a selective apoptosis inducer that increases reactive oxygen species levels to inhibit androgen receptor (AR) and activate p53 pathway. Phenylbutyl isoselenocyanate induces apoptosis in LNCaP prostate cancer cells and has anti-prostate cancer properties.

HY-139970

VPC-13789	Androgen Receptor	Endocrinology Cancer
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC₅₀=0.19 μM) .

HY-164477

FL442	Androgen Receptor	Cancer
FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .

HY-N2908R

Atraric acid (Standard) Methyl atrARate (StandARd)	Reference Standards Androgen Receptor NO Synthase p38 MAPK NF-κB	Inflammation/Immunology Cancer
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-172954

Androgen receptor ligand 1	Androgen Receptor Ligands for Target Protein for PROTAC	Cancer
Androgen receptor ligand 1 is an androgen receptor (AR) ligand. Androgen receptor ligand 1 binds to CRBN E3 ligase via a linker to form an AR PROTAC degrader. Androgen receptor ligand 1 can be used in the study of prostate cancer .

HY-19337S1

Ketodarolutamide-d6 BAY 1896953-d₆; ORM-15341-d₆	Isotope-Labeled Compounds Androgen Receptor	Cancer
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 BAY 1896953-d₃; ORM-15341-d₃	Isotope-Labeled Compounds Androgen Receptor	Cancer
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	Category	Target	Chemical Structure

HY-N2908

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

HY-N0475

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

HY-N2908R

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

Cat. No.	Product Name	Chemical Structure

HY-70002S1

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

HY-70002S

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

HY-16985S

Darolutamide-d4

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

HY-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-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.

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