Signaling Pathway

Androgen Receptor

Androgen Receptor

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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 Inhibitors & Modulators (31)

Product Name Catalog No. Brief Description
3,3'-Diindolylmethane

HY-15758

DIM (3,3'-diindolylmethane), a small molecule compound, is a proposed cancer preventive agent.

Andarine

HY-12023

Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) and an active partial agonist.

ARN-509

HY-16060

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment.

ASC-J9

HY-15194

ASC-J9(GO-Y025; Dimethylcurcumin), is antitumor agent; ASC-J9 suppresses castration-resistant prostate cancer growth via degradation of full-length and splice variant androgen receptors.

AZD3514

HY-16079

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.

Bicalutamide

HY-14249

Bicalutamide(Casodex) is an oral non-steroidal anti-androgen for prostate cancer;  binds to the androgen receptor.

BMS-564929

HY-12111

BMS-564929 is a novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (Ki= 2.11 nM).

Boldenone Undecylenate

HY-17434

Boldenone undecylenate(Equipoise) is a synthetic steroid which has a similar effect as the natural steroid testosterone; it is frequently used in veterinary medicine, though it is also used in humans.

Cortexolone 17 alpha-propionate

HY-13331

Cortexolone 17 alpha-propionate(CB-03-01) is a new topical and peripherally selective androgen antagonist.

Cyproterone acetate

HY-13604

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

Danazol

HY-B1029

Danazol is a derivative of the synthetic steroid ethisterone, that suppresses the production of gonadotrophins, and has some weak androgenic effects.

Dehydroisoandrosterone 3-acetate

HY-B1405

Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.

DHEA

HY-14650

DHEA (Dehydroisoandrosterone) is an important endogenous steroid hormone; DHEA also has a variety of potential biological effects in its own right, binding to an array of nuclear and cell surface receptors and acting as a neurosteroid.

Enzalutamide

HY-70002

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

Epiandrosterone

HY-I0352

Epiandrosterone is a steroid hormone with weak androgenic activity.

Flutamide

HY-B0022

Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

GLPG0492

HY-18102

GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.

GLPG0492 R enantiomer

HY-18102A

GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, which is a novel selective androgen receptor modulator.

GSK-2881078

HY-100186

GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia.

LGD-4033

HY-13981

LGD-4033 is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.