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Results for "

AR-positive

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

2

Natural
Products

1

Isotope-Labeled Compounds

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16985
    Darolutamide
    5+ Cited Publications

    ODM-201; BAY-1841788

    		 Androgen Receptor Cancer
    Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide
  • HY-114402
    ARD-69

    		PROTACs Androgen Receptor Cancer
    ARD-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) .
    ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
    ARD-69
  • HY-N0475
    Triptophenolide

    Hypolide; (+)-Triptophenolide

    		 Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis Inflammation/Immunology Cancer
    Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
    Triptophenolide
  • HY-133045
    VHL Ligand 8

    		Ligands for E3 Ligase Cancer
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
    VHL Ligand 8
  • HY-161369
    CBPD-268

    		PROTACs Histone Acetyltransferase Cancer
    CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
    CBPD-268
  • HY-133020
    ARD-266

    		PROTACs Androgen Receptor Cancer
    ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . ARD-266 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-266
  • HY-16985S
    Darolutamide-d4

    ODM-201-d4; BAY-1841788-d4

    		 Isotope-Labeled Compounds Androgen Receptor Cancer
    Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide-d4
  • HY-164552
    ZNU-IMB-Z15

    		Apoptosis Androgen Receptor Cancer
    ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
    ZNU-IMB-Z15
  • HY-16985R
    Darolutamide (Standard)

    ODM-201 (StandARd); BAY-1841788 (StandARd)

    		 Reference Standards Androgen Receptor Cancer
    Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide (Standard)
  • HY-125065
    MK-4541

    		Androgen Receptor 5 alpha Reductase Endocrinology Cancer
    MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
    MK-4541
  • HY-153519
    WWL0245

    		Epigenetic Reader Domain Cancer
    WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
    WWL0245
  • HY-133044
    Boc-Pip-alkyne-Ph-COOH

    		PROTAC Linkers Cancer
    Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Boc-Pip-alkyne-Ph-COOH
  • HY-121588
    IMTPPE

    		Adrenergic Receptor Cancer
    IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .
    IMTPPE
  • HY-173640
    ID11916

    		Androgen Receptor Phosphodiesterase (PDE) Cancer
    ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .
    ID11916
  • HY-169349
    Androgen receptor antagonist 12

    		Androgen Receptor Cancer
    Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
    Androgen receptor antagonist 12
  • HY-N0475R
    Triptophenolide (Standard)

    Hypolide (StandARd); (+)-Triptophenolide (StandARd)

    		 Reference Standards Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis Inflammation/Immunology Cancer
    Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
    Triptophenolide (Standard)
  • HY-155467
    MRS7935

    		Adenosine Receptor Endocrinology
    MRS7935 (compound 15) is an A1AR positive allosteric modulator (PAM) with an EC50 of approximately 2 μM .
    MRS7935
  • HY-181427
    UT-143

    		Androgen Receptor Cancer
    UT-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 .
    UT-143
  • HY-181971
    XY25028

    		Orphan Nuclear Receptor Androgen Receptor c-Myc Cancer
    XY25028 is an orally active LRH-1 inhibitor with an IC50 of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer .
    XY25028
  • HY-181970
    XY25026

    		Orphan Nuclear Receptor Androgen Receptor c-Myc Cancer
    XY25026 is an orally active LRH-1 inhibitor with an IC50 of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer .
    XY25026
  • HY-77833
    RU 56279

    		Androgen Receptor Drug Metabolite Endocrinology Cancer
    RU 56279 is an androgen receptor (AR) antagonist with strong and systemic anti-androgenic activity. RU 56279 is also a common, potent and long-lasting anti-androgen metabolite of RU 56187 (HY-117486) and RU 58841 (HY-10561) in vivo. RU 56279 can be used as an AR ligand to construct an AR-targeted prodrug system for the study of AR-positive tumor cells .
    RU 56279
  • HY-184124
    JZY3032

    		Androgen Receptor Histone Acetyltransferase Cancer
    JYZ3032 is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JYZ3032 redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JYZ3032 induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JYZ3032 can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer .
    JZY3032
  • HY-184126
    JZY3221

    		Androgen Receptor Cancer
    JZY3221 is an androgen receptor (AR) inhibitor. JZY3221 binds to the AR ligand-binding domain to inhibit AR function. JZY3221 constitutes the AR inhibitory moiety of DALTAC JZY3032 (HY-184124). JZY3221 is applicable to research related to prostate cancer .
    JZY3221

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