Androgen Receptor
Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression. Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. Mutations in this gene are also associated with complete androgen insensitivity (CAIS).
All Product Categories
-
Androgen Receptor Inhibitors
(128)
View all products
-
Androgen Receptor Agonists
(27)
View all products
-
Androgen Receptor Antagonists
(150)
View all products
-
Androgen Receptor Activators
(3)
View all products
-
Androgen Receptor Modulators
(39)
View all products
-
Androgen Receptor Inducer
(1)
View all products
-
Androgen Receptor Degraders
(53)
View all products
-
Androgen Receptor Controls
(3)
View all products
-
Androgen Receptor Ligands
(26)
View all products
-
Androgen Receptor Proteins
(1)
View all products
-
Androgen Receptor Related Products (486)
Related Products (486)
-
Recombinant Proteins (1)
-
Antibodies (2)
-
ATC-324
0 ImagesCat. No.: HY-169385CAS No.: 2925060-81-5ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa. ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
-
AR ligand-39
0 ImagesCat. No.: HY-173373CAS No.: 2156591-18-1AR ligand-39, an androgen receptor (AR) ligand, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). AR ligand-39 can be used for synthesis PROTAC AR Degrader-10 (HY-173372).
-
JJ-450
0 ImagesCat. No.: HY-403733CCAS No.: 2020353-42-6JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant ARF876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as ARF876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003).
-
Acetyl-ACTH (7-24) (human, bovine, rat)
0 ImagesCat. No.: HY-P4786CAS No.: 1815618-01-9Acetyl-ACTH (7-24) (human, bovine, rat) causes a marked decrease of ACTH-evoked corticosterone and aldosterone release.
-
Androgen receptor antagonist 15
0 ImagesCat. No.: HY-184957CAS No.: 3033660-79-3Androgen receptor antagonist 15 is an Androgen receptor (AR) antagonist. Androgen receptor antagonist 15 serves as a Ligand for Target Protein for PROTAC for PROTAC AR degraders, such as ARD-61 (HY-139659). Androgen receptor antagonist 15 is applicable to the research of prostate cancer.
-
Cyproterone Acetate-13C2,d3
0 ImagesCat. No.: HY-W766769Cyproterone Acetate-13C2,d3 is 13C-labeled Cyproterone Acetate (HY-13604).
-
VNPP433-3β hydrochloride
0 ImagesCat. No.: HY-160777BCAS No.: 3026905-91-6Synonyms: Galeterone 3β-imidazole hydrochlorideVNPP433-3β (Galeterone 3β-imidazole) hydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
-
Androgen receptor antagonist 8
0 ImagesCat. No.: HY-153772CAS No.: 1572045-29-4Androgen 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.
-
M17-B15
0 ImagesCat. No.: HY-159739CAS No.: 708291-86-5M17-B15 is an androgen receptor dimerization inhibitor with an IC50 of 30 nM. M17-B15 effectively disrupts AR self-association, thereby suppressing AR signaling. M17-B15 exhibits extraordinary anti- prostate cancer (PCa) efficacy in vitro and in mouse xenograft tumor models.M17-B15 can be used for the study of prostate cancer.
-
Sialorphin
0 ImagesCat. No.: HY-P11642CAS No.: 131748-26-0Sialorphin 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.
-
AR antagonist 17
0 ImagesCat. No.: HY-178148CAS No.: 3064715-04-1AR 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).
-
ERβ agonist-1
0 ImagesCat. No.: HY-173474CAS No.: 2412715-30-9ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer.
-
AR antagonist 11
0 ImagesCat. No.: HY-173409CAS No.: 3005979-40-5AR antagonist 11 (Compound c2) is a selective AR antagonist with an IC50 of 0.019 μM. AR antagonist 11 is also effective against ARF877L/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).
-
Ketodarolutamide-d3
0 ImagesCat. No.: HY-19337SCAS No.: 2484757-41-5Synonyms: BAY 1896953-d3; ORM-15341-d3Ketodarolutamide-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 Ki 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.
-
Androgen receptor degrader-5
0 ImagesCat. No.: HY-162764CAS No.: 2902679-11-0Androgen receptor degrader-5 is an androgen receptor (AR) degrader. Androgen receptor degrader-5 induces proteasome-dependent degradation of androgen receptor protein and inhibits the transcriptional activity of wild-type AR and ARF876L. Androgen receptor degrader-5 exhibits anticancer activity against prostate cancer. Androgen receptor degrader-5 can be used in the research of prostate cancer.
-
Androgen receptor antagonist 3
0 ImagesCat. No.: HY-146026CAS No.: 353484-46-5Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities.
-
VPC-13789
0 ImagesCat. No.: HY-139970CAS No.: 2761146-51-2VPC-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).
-
AR ligand-4
0 ImagesCat. No.: HY-150878CAS No.: 2632308-13-3AR ligand-4 is an androgen receptor (AR) ligand, which can be used for the synthesis of PROTACs, such as ARD-1676 (HY-156111).
-
AR ligand-32
0 ImagesCat. No.: HY-170303CAS No.: 2505498-74-6
