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 Antagonists
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Androgen Receptor Ligands
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Androgen Receptor Proteins
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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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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.
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YXG-158
0 ImagesCat. No.: HY-155666CAS No.: 2952994-34-0YXG‑158 is an orally active, anticancer bifunctional steroid analog with both androgen receptor (AR) degradation activity (DC50 = 1.28 μM) and CYP17A1 inhibitory activity (IC50 = 100 nM). YXG-158 reduces AR protein and mRNA expression via proteasome-dependent degradation, degrades AR-V7, and inhibits CYP17A1 enzymatic activity to block androgen biosynthesis. YXG-158 inhibits the activities of ERα and ERβ, as well as cancer cell proliferation. YXG-158 decreases the weight of androgen-sensitive organs in castrated rats treated with testosterone propionate, downregulates AR protein, reduces PSA levels, and suppresses tumor growth in Enzalutamide (HY-70002)-sensitive and -resistant xenograft models. YXG-158 can be used in prostate cancer-related research.
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AR ligand-33
0 ImagesCat. No.: HY-170330AR ligand-33 is the ligand for androgen receptor, that can be used for synthesis of PROTAC AR Degrader-8 (HY-170329) as the target protein ligand.
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BMS-779333
0 ImagesCat. No.: HY-119170CAS No.: 1095181-60-4BMS-779333 is an orally active androgen receptor (AR) antagonist. BMS-779333 is promising for research of prostate cancer and seizure.
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AR ligand-38
0 ImagesCat. No.: HY-170450AR ligand-38 is the ligand for androgen receptor, that can be used for synthesis of PROTAC AR Degrader-9 (HY-170448).
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AR antagonist 4
0 ImagesCat. No.: HY-151266CAS No.: 2883447-45-6AR antagonist 4 is an orally active androgen receptor (AR) antagonist with a DC50 of 2.84 μM in LNCaP human prostate cancer cells. AR antagonist 4 inhibits dihydrotestosterone-induced AR transcriptional activity, promotes proteasome-dependent AR degradation, and dose-dependently promotes AR-V7 degradation. AR antagonist 4 can be used for the research of metastatic castration-resistant prostate cancer.
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CBP/p300-IN-25
0 ImagesCat. No.: HY-185786CAS No.: 3105154-92-2CBP/p300-IN-25 is a CBP/p300 heterobifunctional conditional inhibitor. CBP/p300-IN-25 mediates conditional CBP/p300 inhibition through simultaneous binding to CBP/p300 and AR. CBP/p300-IN-25 is applicable to the research of prostate cancer.
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PROTAC AR Degrader-7
0 ImagesCat. No.: HY-160221CAS No.: 2505495-83-8PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting androgen receptor with an IC50 value of 3 nM.
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S-40503
0 ImagesCat. No.: HY-103578CAS No.: 404920-28-1S-40503 is a tissue-selective androgen receptor (AR) agonist with a Ki of 14.9 nM for rat AR. S-40503 binds to AR with high specificity, exerts full agonistic effects in bone and muscle, acts as a partial agonist in the prostate, and preferentially targets anabolic tissues rather than androgen-dependent tissues. S-40503 can be used in the research of osteoporosis.
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3'-Hydroxy stanozolol
0 ImagesCat. No.: HY-138151CAS No.: 125709-39-93'-Hydroxy stanozolol is a major metabolite of the anabolic androgenic steroid Stanozolol.
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(R)-Bicalutamide-d5
0 ImagesCat. No.: HY-14249S1(R)-Bicalutamide-d5 is deuterated labeled (R)-Bicalutamide (HY-108250). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
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AR/AR-V7-IN-1
0 ImagesCat. No.: HY-163510CAS No.: 2964558-54-9AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer.
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TD-802
0 ImagesCat. No.: HY-146397CAS No.: 2760703-21-5TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models.
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RLA-5331
0 ImagesCat. No.: HY-152520RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line.
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Galeterone hydrochloride
0 ImagesCat. No.: HY-70006ACAS No.: 1239339-17-3Synonyms: TOK-001 hydrochloride; VN-124-1 hydrochlorideGaleterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].
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Androgen receptor antagonist-14
0 ImagesCat. No.: HY-183287Androgen receptor antagonist-14 (Compound S-94) is a selective antagonist of the T878A mutant androgen receptor (AR) with an IC50 of 0.38 μM. Androgen receptor antagonist-14 selectively antagonizes the transcriptional activity of the ART878A, ARF877L/T878A and ARH875Y/T878A mutant androgen receptors. Androgen receptor antagonist-14 exhibits anticancer activity against prostate cancer. Androgen receptor antagonist-14 can be used in the research of prostate cancer.
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Di(5-(methylsulfonyl)-1,3,4-oxadiazol-2-yl)-benzene-amide-PEG4-ester-2,3,5,6-F-Ph
0 ImagesCat. No.: HY-176863CAS No.: 3094598-90-7Di(5-(methylsulfonyl)-1,3,4-oxadiazol-2-yl)-benzene-amide-PEG4-ester-2,3,5,6-F-Ph (Compound L-1026) is a linker that connects Androgen Receptor (AR) RNAi agent to targeting ligands (such as antibodies). The conjugation can inhibit AR gene expression and reduce AR activity. Di(5-(methylsulfonyl)-1,3,4-oxadiazol-2-yl)-benzene-amide-PEG4-ester-2,3,5,6-F-Ph can be used for spinal and bulbar muscular atrophy (SBMA) research.
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AR ligand-44
0 ImagesCat. No.: HY-400666CAS No.: 2632308-15-5AR ligand-44 is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051 (HY-149862).
