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 (486)
Related Products (486)
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Recombinant Proteins (1)
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Antibodies (2)
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AR Degrader-3
0 ImagesCat. No.: HY-178938CAS No.: 1182011-65-9AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC).
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AR ligand-44 TFA
0 ImagesCat. No.: HY-400666AAR ligand-44 TFA is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051 (HY-149862).
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Apalutamide-d7
0 ImagesCat. No.: HY-16060S3Synonyms: ARN-509-d7Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
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Lupeol-d3
0 ImagesCat. No.: HY-W744741Lupeol-d3 is the deuterium labeled Lupeol (HY-N0790). Lupeol is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor?(AR)?inhibitor and can be used for?cancer?research, especially prostate?cancer?of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
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YM580
0 ImagesCat. No.: HY-180409CAS No.: 262295-11-4YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC50 = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (Kis > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer.
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Ch-319
0 ImagesCat. No.: HY-122894CAS No.: 2589088-07-1Ch-319 is a Triphenyltin (IV) carboxylate derivative. Ch-319 reduces androgen receptor expression, AKT and PRAS40 phosphorylation levels, and increases FOXO3a expression. Ch-319 increases Apoptosis. Ch-319 can be used in the research of prostate cancer.
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WH23
0 ImagesCat. No.: HY-181670WH23 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 μM. WH23 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. WH23 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. WH23 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. WH23 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. WH23 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer.
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EST1140
0 ImagesCat. No.: HY-187458CAS No.: 3105892-11-0EST1140 is a covalent molecular glue degrader targeting RNF126 for AR/AR-V7, with DC50 values of 33 μM and 30 μM, respectively, in 22Rv1 cells. EST1140 covalently binds to the E3 ligase RNF126 to achieve targeted protein degradation. EST1140 can be used in the research of androgen-independent prostate cancer.
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Anticancer agent 135
0 ImagesCat. No.: HY-155543CAS No.: 2957914-60-0Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models.
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Boc-Glycine-2-13C
0 ImagesCat. No.: HY-Y0978S2CAS No.: 145143-02-8Synonyms: N-tert-Butoxycarbonyl-2-aminoacetic acid-2-13C; NSC 127669-2-13CBoc-Glycine-2-13C is a 13C-labeled Boc-Glycine (HY-Y0978). Boc-Glycine is a Glycine (HY-Y0966) derivative.
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Brassicasterol (Standard)
0 ImagesCat. No.: HY-113289RCAS No.: 474-67-9L-Ornithine (hydrochloride) (Standard) is the analytical standard of L-Ornithine (hydrochloride). This product is intended for research and analytical applications. L-Ornithine hydrochloride is a non-proteinogenic amino acid, is mainly used in urea cycle removing excess nitrogen in vivo. L-Ornithine hydrochloride shows nephroprotective.
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RU 58642
0 ImagesCat. No.: HY-120703CAS No.: 143782-63-2RU 58642 is an orally active non-steroidal antiandrogen, which displays a strong and selective affinity for androgen receptor.
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KF-19418
0 ImagesCat. No.: HY-167655CAS No.: 147508-06-3KF-19418 is a hair follicle stimulator with hair growth promoting activity. KF-19418 stimulates proliferation of cultured hair bulb cells from newborn mice. KF-19418 accelerates hair regrowth in hair-clipped mouse alopecia model following topical application. KF-19418 can be used for the research of alopecia.
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GSK-3β/G9a-IN-1
0 ImagesCat. No.: HY-W657887CAS No.: 154866-92-9GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease.
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AR antagonist 5
0 ImagesCat. No.: HY-157455CAS No.: 2902679-53-0AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure[1.
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PeS-9
0 ImagesCat. No.: HY-174377PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.
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A031
0 ImagesCat. No.: HY-148777CAS No.: 2682255-44-1A031 is a PROTAC degrader targeting the androgen receptor. A031 induces time-dependent degradation of androgen receptor protein. A031 exerts tumor growth inhibitory effects in a zebrafish model xenografted with human prostate cancer cells. A031 can be used in studies related to prostate cancer.
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Atriopeptin I (rat, mouse)
0 ImagesCat. No.: HY-P10248CAS No.: 89139-53-7Atriopeptin I rat, mouse is an atrial natriuretic peptide, which stimulates the testosterone production with half-maximum stimulation of 38 nM.
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NEP28
0 ImagesCat. No.: HY-156059CAS No.: 1254176-87-8NEP28 is a selective androgen receptor modulator with an EC50 of 2.90 nM in 22RV1 cells. NEP28 increases the activity of Aβ-degrading enzyme neprilysin. NEP28 is efficacious in muscle and brain without serious side effects on prostate in rats. NEP28 can be used for osteoporosis, sarcopenia, and Alzheimer's disease research.
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YM-1758735
0 ImagesCat. No.: HY-180410CAS No.: 262294-30-4YM-1758735 is an orally active androgen receptor (AR) antagonist with an IC50 of 0.2 μM. YM-1758735 inhibits AR-mediated transcriptional activation. YM-1758735 can be used for the research of prostate.
