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 Related Products (483)
Related Products (483)
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Recombinant Proteins (1)
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Antibodies (2)
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VPC-14228
0 ImagesVPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer[2].
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Atraric acid
0 ImagesAtraric 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.
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Pfn1-IN-1
0 ImagesPfn1-IN-1 (compound C1) is a Pfn1 inhibitor that inhibits the angiogenic capacity of endothelial cells (EC). Pfn1 is a regulator of the actin cytoskeleton, inducing actin polymerization and essential cellular activities. Pfn1-IN-1 inhibits Pfn1-Actin interaction and Actin polymerization.
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Hydroxyflutamide
0 ImagesSynonyms: HFTHydroxyflutamide (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC50 of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases.
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Ar-V7-IN-1
0 ImagesAr-V7-IN-1 is a potent inhibitor of Ar-V7. Ar-V7-IN-1 inhibits the transcriptional activity of androgen receptor (AR) and the secretion of prostate-specific antigen (PSA) with an eGFP IC50 of 1232 nM and the PSA IC50 of 1391 μM. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer.
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ARD-2585
0 ImagesARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
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ACP-105
0 ImagesACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
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Alternariol
0 ImagesAlternariol 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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Brassicasterol
0 ImagesBrassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease.
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RU 58841
0 ImagesSynonyms: PSK-3841; HMR-3841RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 has a dramatic effect on hair regrowth.
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Medroxyprogesterone acetate (Standard)
0 ImagesSynonyms: Medroxyprogesterone 17-acetate(Standard); Farlutin (Standard)Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
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AC-262536
0 ImagesAC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM).
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GSK-2881078
0 ImagesGSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness.
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ARD-69
0 ImagesARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC).
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ARD-2128
0 ImagesARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
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Enzalutamide-d6
0 ImagesSynonyms: MDV3100-d6Enzalutamide-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.
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Leelamine hydrochloride
0 ImagesLeelamine hydrochloride is an orally active weakly basic amine that inhibits NPC1 and the androgen receptor AR-V7, and acts as a cannabinoid receptor agonist. Leelamine hydrochloride also functions as a lysosome affinity agent that blocks endocytosis, disrupts autophagic flux and cholesterol transport, thereby altering the RTK-AKT/STAT/MAPK signaling cascade. Leelamine hydrochloride induces cancer cell death and autophagosome accumulation, and can be used in research related to melanoma, castration-resistant prostate cancer and breast cancer.
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GDC-2992
0 ImagesSynonyms: RO7656594GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study.
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LY2452473
0 ImagesLY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
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(R)-Bicalutamide
0 Images(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
