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).
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Androgen Receptor Inhibitors
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Androgen Receptor Ligands
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Androgen Receptor Related Products (486)
Related Products (486)
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Recombinant Proteins (1)
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Antibodies (2)
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Torulene
0 ImagesTorulene (Torulin) is an orally active carotenoid with anti-cancer activity. Torulene inhibits proliferation and induces apoptosis of tumor cells via a mitochondrial signal pathway and the down-regulation of androgen receptor (AR) expression. Torulene can be used for the study of prostate cancer.
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EPI-001 (Standard)
0 ImagesCat. No.: HY-100348RCAS No.: 227947-06-0EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
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LG-121071
0 ImagesCat. No.: HY-103577CAS No.: 179897-70-2LG-121071 is an orally active and selective androgen receptor modulator with a Ki of 17 nM.
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AR ligand-37
0 ImagesCat. No.: HY-168697AR ligand-37 is a PROTAC target protein ligand that can be used to synthesize BMS-986365 (HY-158101).
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RU 59063
0 ImagesRU 59063 is a high-affinity, selective nonsteroidal androgen receptor (AR) ligand that acts as a partial AR agonist/antagonist in CV-1 cell transcription assays. RU 59063 has a Ka value of 6.2×109 M-1 for human AR. RU 59063 induces a conformation of AR that can bind to the androgen response element (ARE), triggers partial AR-dependent transcriptional activation, and antagonizes testosterone-induced AR transcriptional activity. RU 59063 inhibits testosterone propionate-induced ornithine decarboxylase activity in mouse kidneys and testosterone propionate-induced prostate weight gain in rats. RU 59063 can be used in studies related to prostate cancer.
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Psa-AR
0 ImagesCat. No.: HY-179056Psa-AR is a PROTAC degrader targeting PSMA, with a Kd of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer.
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3-Oxochol-5-en-24-oic acid
0 ImagesCat. No.: HY-179476CAS No.: 847232-54-63-Oxochol-5-en-24-oic acid is a rare bile acid produced by the intestinal microbiota. 3-Oxochol-5-en-24-oic acid is a potent antagonist of the human androgen receptor (hAR), with an IC50 of 119.4 nM. 3-Oxochol-5-en-24-oic acid has no significant agonistic or antagonistic effects on estrogen receptors (ER) or glucocorticoid receptors (GR). 3-Oxochol-5-en-24-oic acid effectively inhibits the growth of prostate cancer cells. In animal models, it enhances the efficacy of anti-PD-1 therapy by regulating the differentiation of CD8+ T cells. 3-Oxochol-5-en-24-oic acid can be used for research on regulating host immunity and anti-tumor studies.
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(Des-Glu5)-ACTH (1-24) (human, bovine, rat)
0 ImagesCat. No.: HY-P4413CAS No.: 1815617-95-8(Des-Glu5)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production.
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Vinclozolin
0 ImagesVinclozolin is a non-systemic dicarboximide fungicide. Vinclozolin is also an antagonist of the androgen receptor, exerting anti-androgenic effects through its metabolites. Vinclozolin inhibits spore germination and can be used to control fungi in plants such as vegetables and fruits. Vinclozolin is toxic to the reproductive system of rats and possesses certain anti-tumor activity.
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Acetyl-ACTH (4-24) (human, bovine, rat)
0 ImagesCat. No.: HY-P4784CAS No.: 1815618-00-8Acetyl-ACTH (4-24) (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.
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3βHSD1-IN-1
0 ImagesCat. No.: HY-174244CAS No.: 3082852-63-63βHSD1-IN-1 (Compound 46) is a 3β-hydroxysteroid dehydrogenase 1 (3βHSD1) inhibitor with an IC50 of 55 nM. 3βHSD1-IN-1 can effectively inhibit androgen receptor activity. 3βHSD1-IN-1 can be used in the research of diseases such as prostate cancer.
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Alternariol (Standard)
0 ImagesAlternariol (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.
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MeSeI
0 ImagesCat. No.: HY-159106CAS No.: 2901664-87-5MeSeI exhibits a weak inhibitory activity against monoamine oxidase MAO-A and MAO-B (IC50=198.8 µM). MeSeI regulates dopamine receptor D2 and norepinephrine receptor α2, β1, and exhibits antidepressant-like effect in mice. MeSeI is orally active.
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Isosilybin B (Standard)
0 ImagesCat. No.: HY-N7045RCAS No.: 142796-22-3Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
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p-Hydroxyphenylacetone
0 ImagesCat. No.: HY-W087006CAS No.: 770-39-8p-Hydroxyphenylacetone, a Raspberry ketone (HY-N1426) derivative, is an androgen receptor (AR) antagonist with an IC50 of 420 μM in MDA-kb2 human breast cancer cells. p-Hydroxyphenylacetone can be used for breast cancer research.
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ZC9
0 ImagesCat. No.: HY-179123CAS No.: 2757513-79-2ZC9 is a androgen receptor (AR) molecular glue degrader. ZC9 directly binds to AR and inhibits Dihydrotestosterone-induced nuclear translocation of AR. ZC9 promotes AR degradation via the ubiquitin-proteasome system and suppresses AR transcriptional activity. ZC9 significantly decreases the mRNA levels of other AR downstream genes, including PSA, TMPRSS2, and PMEPA1. ZC9 promotes Apoptosis. ZC9 exhibits anticancer activity against prostate cancer.
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VPC-3033
0 ImagesCat. No.: HY-118409CAS No.: 110763-24-1VPC-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).
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Bisphenol F bis(2-chloro-1-propanol) ether
0 ImagesCat. No.: HY-W585917CAS No.: 374772-79-9Synonyms: BFDGE·2HClBisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) is an androgen receptor antagonist with a human IC50 of 18 μM. Bisphenol F bis(2-chloro-1-propanol) ether binds to the androgen receptor. Bisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) can be used for research on hormonal activity.
