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 Agonists
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Androgen Receptor Antagonists
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Androgen Receptor Ligands
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Androgen Receptor Proteins
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Androgen Receptor Related Products (476)
Related Products (476)
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Recombinant Proteins (1)
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Antibodies (2)
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4-sec-Butylphenol
0 ImagesCat. No.: HY-W142795CAS No.: 99-71-8Synonyms: 4-sec-BP4-sec-Butylphenol (4-sec-BP) is an androgen receptor ligand that binds to the androgen receptor with a pIC50 of 4.07. 4-sec-Butylphenol is an estrogen receptor agonist. 4-sec-Butylphenol can be found in industrial effluents, in production water of oil and gas platforms, as well as in river water samples.
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ChEMBL22003
0 ImagesCat. No.: HY-176048CAS No.: 152813-63-3ChEMBL22003 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.
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PROTAC AR Degrader-9
0 ImagesCat. No.: HY-170448PROTAC AR Degrader-9 is a topically applicable androgen receptor (AR) PROTAC degrader. PROTAC AR Degrader-9 recruits Cereblon (CRBN) E3 ubiquitin ligase to induce AR ubiquitination and proteasomal degradation in human dermal papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 possesses excellent skin retention, modulates androgenetic alopecia (AGA)-related downstream paracrine factors including TGF-β1 and β-catenin, promotes hair regeneration in mice. and exhibits favorable skin pharmacokinetics profiles with minimal systemic exposure. PROTAC AR Degrader-9 can be used for the study of androgenetic alopecia (AGA).
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CDK9-IN-50
0 ImagesCat. No.: HY-183710CAS No.: 3114520-65-6CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC50 of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer.
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AR Degrader-1
0 ImagesCat. No.: HY-163641AR Degrader-1 is a molecular glue degrader targeting the androgen receptor (AR). AR Degrader-1 induces androgen receptor degradation by recruiting the DCAF16 E3 ligase substrate receptor, thereby triggering ubiquitination and proteasomal degradation. AR Degrader-1 exhibits relatively selective degradation of the androgen receptor in prostate cancer cells, reducing the levels of only a small number of other proteins. AR Degrader-1 can be used in studies related to prostate cancer.
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AR antagonist 15
0 ImagesCat. No.: HY-174391CAS No.: 1790308-86-9AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. 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.
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PROTAC AR/BET protein degrader-1
0 ImagesCat. No.: HY-160262CAS No.: 2571123-81-2PROTAC 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.
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Androgen receptor antagonist 13
0 ImagesCat. No.: HY-172908CAS No.: 2558183-91-6Androgen 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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HEMTAC AR degrader-1
0 ImagesCat. No.: HY-187229HEMTAC AR degrader-1 is an androgen receptor (AR) HEMTAC degrader that recruits HSP70, with a Kd value of 825 nM for HSP72. HEMTAC AR degrader-1 induces AR degradation, and inhibits the proliferation and migration of cancer cells. HEMTAC AR degrader-1 can be used in the research of prostate cancer.
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Procyanidin B3 (Standard)
0 ImagesCat. No.: HY-N2345RCAS No.: 23567-23-9Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
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2,2,5,7,8-Pentamethyl-6-Chromanol (Standard)
0 ImagesSynonyms: PMC (Standard)2,2,5,7,8-Pentamethyl-6-Chromanol (Standard) is the analytical standard of 2,2,5,7,8-Pentamethyl-6-Chromanol. This product is intended for research and analytical applications. 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines[1].
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AR antagonist 8
0 ImagesCat. No.: HY-163485CAS No.: 3036567-30-0AR antagonist 8 (compound 16), an unnatural entestrane, is a potent Lupeol-inspired androgen receptor (AR) antagonist with an IC50 of 0.76 μM.
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Flutamide-d7
0 ImagesCat. No.: HY-B0022SCAS No.: 223134-72-3Synonyms: SCH 13521-d7Flutamide-d7 is deuterium labeled Flutamide.
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β-catenin inhibitory peptoid
0 ImagesCat. No.: HY-P11007CAS No.: 2579070-02-1β-catenin inhibitory peptoid (compound 13) inhibits the β-catenin:TCF interaction with an IC50 of 5.44 µM. β-catenin inhibitory peptoid inhibits both Wnt (IC50 of 0.105 µM) and androgen receptor (AR)-signaling (IC50 of 1.02 µM) in prostate cancer cell lines. β-catenin inhibitory peptoid markedly diminishes cell proliferation of prostate cancer cell lines.
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(–)-JJ-450
0 ImagesCat. No.: HY-403733ACAS No.: 1998094-23-7(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant ARF876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide.
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PROTAC AR-NTD degrader 1
0 ImagesCat. No.: HY-149434CAS No.: 3032601-92-3PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively.
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Bicalutamide sulfide
0 ImagesCat. No.: HY-W102330CAS No.: 90356-78-8Bicalutamide sulfide (compound 39) is a nonsteroidal antiandrogen. Bicalutamide sulfide can be used for the study of androgen-responsive benign and malignant disease.
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Ketodarolutamide-d6
0 ImagesCat. No.: HY-19337S1Synonyms: BAY 1896953-d6; ORM-15341-d6Ketodarolutamide-d6 (BAY 1896953-d6) 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.
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UT-143
0 ImagesCat. No.: HY-181427CAS No.: 2698320-33-9UT-143 is an orally active, selective irreversible covalent antagonist of androgen receptor (AR). UT-143 inhibits the proliferation of AR-positive prostate cancer cells, reduces the weight of androgen target tissues in rats, and suppresses the growth of AR-positive xenograft tumors. UT-143 can be used for the research of prostate cancer.
