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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
26 Results for "
inhibits AR nuclear translocation
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "inhibits AR nuclear translocation" in MCE Product Catalog:
13
13 Publications Verification
Cat. No.: HY-16985
CAS No.: 1297538-32-9
Synonyms: ODM-201; BAY-1841788
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Research Areas:
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 .
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5 Cited Publications
Cat. No.: HY-N5124
CAS No.: 60767-80-8
Synonyms: Isovitexin 2''-O-glucoside; Isovitexin 2''-O-β-D-glucoside
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2
2 Cited Publications
Synonyms: Ordenina hydrochloride; Peyocactine hydrochloride
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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 .
Cat. No.: HY-N0475
CAS No.: 74285-86-2
Synonyms: Hypolide; (+)-Triptophenolide
Cat. No.: HY-164373
CAS No.: 1898232-70-6
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SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
Cat. No.: HY-16985S
CAS No.: 2484757-20-0
Synonyms: ODM-201-d4; BAY-1841788-d4
Cat. No.: HY-16985R
CAS No.: 1297538-32-9
Synonyms: ODM-201 (StandARd); BAY-1841788 (StandARd)
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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 .
Cat. No.: HY-N0113S
CAS No.: 1346598-66-0
Synonyms: Ordenina-d6; Peyocactine-d6
Target:
Isotope-Labeled Compounds Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Hordenine-d6 (Ordenina-d6; Peyocactine-d6) is the deuterated-labeled Hordenine (HY-N0113). Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder .
Cat. No.: HY-179123
CAS No.: 2757513-79-2
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ZC9 is a androgen receptor (AR) molecular glue degrader. ZC9 directly binds to AR and inhibits Dihydrotestosterone-induced nuclear translocation of AR. ZC9 promotes AR degradation via the ubiquitin-proteasome system and suppresses AR transcriptional activity. ZC9 significantly decreases the mRNA levels of other AR downstream genes, including PSA, TMPRSS2, and PMEPA1. ZC9 promotes Apoptosis. ZC9 exhibits anticancer activity against prostate cancer .
Cat. No.: HY-155543
CAS No.: 2957914-60-0
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Anticancer 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 .
Cat. No.: HY-403733A
CAS No.: 1998094-23-7
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(-)-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 AR F876L 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 .
Cat. No.: HY-178148
CAS No.: 3064715-04-1
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AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .
Cat. No.: HY-403733C
CAS No.: 2020353-42-6
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JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR F876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .
Cat. No.: HY-173640
CAS No.: 2785317-21-5
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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 .
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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 .
Cat. No.: HY-N0475R
CAS No.: 74285-86-2
Synonyms: Hypolide (StandARd); (+)-Triptophenolide (StandARd)
Cat. No.: HY-N0113BR
CAS No.: 6027-23-2
Synonyms: Ordenina hydrochloride (StandARd); Peyocactine hydrochloride (StandARd)
Category:
Coryphantha vivipara var arizonica Alkaloids Cactaceae Extract Monophenols Other Alkaloids Phenols Plants
Target:
Reference Standards Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Cat. No.: HY-N0113BS
Synonyms: Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride
Target:
Isotope-Labeled Compounds Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Research Areas:
Hordenine-d6 hydrochloride (Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride) is the deuterated-labeled Hordenine hydrochloride (HY-N0113B). Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
