Androgen Receptor

Related Products

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).

Androgen Receptor Related Products (340)
Recombinant Proteins (1)
Antibodies (2)

By Effects:	Controls (2) Inhibitors (91) Ligands (3) Agonists (25) Degraders (26) Antagonists (112) Activators (3) Modulators (36) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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-152850A

Gumelutamide monosuccinate	Antagonist
Gumelutamide (monosuccinate) is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide (monosuccinate) is an androgen antagonist.

HY-122611R

CSRM617 (Standard)	Inhibitor
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-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-W745855

Androstatrione
Androstatrione is an androgenic compound.

HY-106827

Trimegestone	Inhibitor
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-P4779

Acetyl-ACTH (2-24) (human, bovine, rat)	Modulator
Acetyl-ACTH (2-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor.

HY-135473S

Chlormadinone-d₆	Inhibitor
Chlormadinone-d₆ is the deuterium labeled Chlormadinone (HY-135473) . Chlormadinone is an antiandrogen agent. Chlormadinone can be used for the study of benign prostatic hyperplasia (BPH).

HY-156751

(Rac)-GDC-2992	Degrader
(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-163813

AR Degrader-2	Degrader
AR Degrader-2 (Compound 2) is a molecular glue that degrades androgen receptor (AR) with a DC₅₀ of 0.3-0.5 μM in cell VCaP.

HY-157491

K2-B4-5e	Degrader
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-W013272R

Hydroxyflutamide (Standard)	Antagonist
Hydroxyflutamide (Standard) is the analytical standard of Hydroxyflutamide. This product is intended for research and analytical applications. Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer.

HY-176128

BWA-6047	Degrader
BWA-6047 is a dual AR/AR-V7 and GSPT1 PROTAC degrader (AR: DC₅₀ = 3.7 nM; AR-V7: DC₅₀ = 3.0 nM; GSPT1: DC₅₀ = 1.2 nM). BWA-6047 promotes ubiquitination and degradation of AR/AR-V7 and, through its molecular glue properties, induces the formation of a PPI between GSPT1 and CRBN, leading to GSPT1 degradation. BWA-6047 can be used in prostate cancer research (Pink: AR/AR-V7 ligand (HY-176129); Blue: E3 CRBN ligand (HY-W069604); Black: linker (HY-W069604)).

HY-126464

Estromustine	Modulator
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-176048

ChEMBL22003	Modulator
ChEMBL22003 is a potential phase separation modulator of ARV7 that can bind to the ARV7 binding sites. ChEMBL22003 has potential for use in the research of prostate cancer.

HY-170448

PROTAC AR Degrader-9	Degrader
PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC₅₀ of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models. (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))

HY-163641

AR Degrader-1	Degrader
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-174391

AR antagonist 15	Inducer
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^[1].

HY-160262

AR/BET protein degrader-1	Degrader
AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research.

HY-172908

Androgen receptor antagonist 13	Antagonist
Androgen receptor antagonist 13 (compound 8a) is an orally active Androgen receptor antagonist with an IC₅₀ of 0.20 μM. Androgen receptor antagonist 13 can be used in the study of prostate cancer.

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Androgen Receptor

Androgen Receptor

Androgen Receptor Related Products (340)

Recombinant Proteins (1)

Antibodies (2)

Androgen Receptor Related Products (340):