2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Androgen Receptor

Androgen Receptor

Androgen Receptor

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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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1978
    Iprodione
    		Inhibitor 99.25%
    Iprodione is an orally active diformimide fungicide. Iprodione can specifically cause oxidative damage by producing free radicals (ROS). Iprodione is also an antiandrogen agent that delays adolescent development in rats and reduces sexual behavior and reproductive ability in rats.
    Iprodione
  • HY-103245
    Cl-4AS-1
    		Agonist 99.64%
    Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).
    Cl-4AS-1
  • HY-149862
    ARD-2051
    		98.19%
    ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer.
    ARD-2051
  • HY-16060S
    Apalutamide-d4
    		Antagonist 99.90%
    Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-d<sub>4</sub>
  • HY-109619
    D4-abiraterone
    		Antagonist 99.75%
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
    D4-abiraterone
  • HY-160777
    VNPP433-3β
    		Degrader 98.01%
    VNPP433-3β (Galeterone 3β-imidazole) is an 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.VNPP433-3β induces cell apoptosis. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
    VNPP433-3β
  • HY-141487
    CLP-3094
    		Inhibitor 99.92%
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
    CLP-3094
  • HY-116895
    JJH260
    		Inhibitor 98.05%
    JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively.
    JJH260
  • HY-160020
    ET516
    		Inhibitor 99.13%
    ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants.
    ET516
  • HY-14250
    PF-998425
    		Antagonist 98.31%
    PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research.
    PF-998425
  • HY-B1866
    Linuron
    		Antagonist 99.88%
    Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
    Linuron
  • HY-13607
    BMS-641988
    		Antagonist 98.76%
    BMS-641988 (compound 23) is an oral active nonsteroidal androgen receptor antagonist with the Ki of 1.7 nM. BMS-641988 shows anticancer activity.
    BMS-641988
  • HY-103576
    LGD-3303
    		Modulator 99.57%
    LGD-3303 is a selective androgen receptor modulator (SARM).
    LGD-3303
  • HY-135732
    SK33
    		Antagonist 99.98%
    SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity.
    SK33
  • HY-164807
    SARD279
    		Degrader
    SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research.(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
    SARD279
  • HY-B1986
    p,p'-DDE
    		Antagonist 99.51%
    p,p'-DDE (4,4'-DDE) is the major and persistent metabolite of DDT. p,p'-DDE is a orally active androgen receptor antagonist with an IC50 of 5 μM and a Ki of 3.5 μM. p,p'-DDE can affect the development and function of the male reproductive system. Additionally, high serum concentrations of p,p'-DDE may be a risk factor for type 2 diabetes in women.
    p,p'-DDE
  • HY-161741
    VinclozolinM2-2204
    		Degrader 98.00%
    VinclozolinM2-2204 is a androgen receptor (AR) AUTOTAC degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR+LC3+ autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer.(Pink: AR inhibitor (HY-168296); Black: linker (HY-128833); Blue: CRBN Ligand (HY-168293))
    VinclozolinM2-2204
  • HY-130845A
    AR antagonist 1 hydrochloride
    		Antagonist 99.53%
    AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1 hydrochloride
  • HY-139659
    ARD-61
    		Inhibitor 99.68%
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-61
  • HY-123047
    Tibolone
    		Agonist 99.39%
    Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity