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Results for "

AR signaling

" in MedChemExpress (MCE) Product Catalog:

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16985
    Darolutamide
    Maximum Cited Publications
    8 Publications Verification

    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-158101
    BMS-986365
    1 Publications Verification

    CC-94676

    		 PROTACs Androgen Receptor Cancer
    BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .
    BMS-986365
  • HY-N0138
    Theobromine
    1 Publications Verification

    3,7-Dimethylxanthine

    		 Adenosine Receptor Endogenous Metabolite Neurological Disease
    Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
    Theobromine
  • HY-N2037
    Higenamine
    Maximum Cited Publications
    8 Publications Verification

    Norcoclaurine; Demethyl-Coclaurine

    		 MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis Cardiovascular Disease Endocrinology
    Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
    Higenamine
  • HY-N2908
    Atraric acid

    Methyl atrARate

    		 Environmental Pollutants NF-κB Androgen Receptor p38 MAPK NO Synthase Inflammation/Immunology Cancer
    Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .
    Atraric acid
  • HY-116522
    AR420626
    4 Publications Verification

    		 Free Fatty Acid Receptor Histone Methyltransferase HDAC mTOR CaMK p38 MAPK Epigenetic Reader Domain GLUT nAChR TNF Receptor Metabolic Disease Inflammation/Immunology Cancer
    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca 2+ signal-mediated glucose uptake and improve diabetes .
    AR420626
  • HY-N0819
    Raddeanin A
    1 Publications Verification

    		 Apoptosis PI3K Akt ERK mTOR Wnt β-catenin Wee1 JNK VEGFR CDK Neurological Disease Inflammation/Immunology Cancer
    Raddeanin A is an oleanane-type triterpenoid saponin with oral activity. Raddeanin A inhibits SRC, mTOR, JNK, VEGFR2, NLRP3 inflammasome, Wnt/β-catenin, Wee1, PI3K/AKT signaling pathway, MAPK/ERK signaling pathway, AR-FL, AR-Vs, and downregulates the expression of p-PI3K and p-AKT. Raddeanin A inhibits osteoclast formation, bone resorption, osteolysis, cancer cell invasion, migration, proliferation, angiogenesis and epithelial-mesenchymal transition, while induces apoptosis, cell cycle arrest, ROS production, immunogenic cell death and dendritic cell maturation. Raddeanin A improves blood-retinal barrier function, alleviates inflammation, regulates the tumor microenvironment, and enhances the activity of anti-PD-1 antibody. Raddeanin A is applicable to the research of breast cancer-associated osteolysis, human osteosarcoma, colorectal cancer, glioblastoma, Alzheimer's disease, cholangiocarcinoma, melanoma, non-small cell lung cancer, castration-resistant prostate cancer and multiple myeloma .
    Raddeanin A
  • HY-16079
    AZD3514
    3 Publications Verification

    		 Androgen Receptor Cancer
    AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer .
    AZD3514
  • 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-171978
    LM-189

    		Adrenergic Receptor Cardiovascular Disease
    LM-189 is a β2-adrenergic receptor (β2AR) ligand and G protein-biased modulator with a human β2AR Ki of 0.063 nM.LM-189 promotes β2AR coupling to Gαs and Gαi heterotrimers, stabilizes distinct β2AR conformations including a TM6 outward state, and increases β2AR ICL2 dynamics.LM-189 restricts β2AR ligand-binding pocket conformational heterogeneity, stabilizes polar ligand-receptor interaction networks, and exhibits bias toward Gαi signaling over Gαs signaling.LM-189 enabled cryo-EM structural characterization of the β2AR-Gi complex.LM-189 can be used for the research of congestive heart failure .
    LM-189
  • HY-149433
    BWA-522

    		PROTACs Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .
    BWA-522
  • HY-19319
    MI-136
    1 Publications Verification

    		 Epigenetic Reader Domain Androgen Receptor Apoptosis Cancer
    MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors .
    MI-136
  • HY-111024
    2,2,5,7,8-Pentamethyl-6-Chromanol

    PMC

    		 Androgen Receptor NF-κB Cardiovascular Disease Inflammation/Immunology Cancer
    2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines .
    2,2,5,7,8-Pentamethyl-6-Chromanol
  • HY-N7043
    Isosilybin A
    2 Publications Verification

    		 Apoptosis PPAR NF-κB p38 MAPK ERK Androgen Receptor Inflammation/Immunology Cancer
    Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity [1][2][3].
    Isosilybin A
  • HY-159190
    HRX-0233

    		MAPKAPK2 (MK2) Cancer
    HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
    HRX-0233
  • HY-120006A
    (rel)-AR234960
    1 Publications Verification

    		 ERK Cardiovascular Disease
    (rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS. (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor (CTGF) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor. (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure .
    (rel)-AR234960
  • HY-162702
    AZ'3137

    		PROTACs Androgen Receptor Cancer
    AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Pink: AR Ligand (HY-172954); Blue: CRBN ligand (HY-172955); Black: linker (HY-W262798); E3 Ligand+Linker: HY-172956) .
    AZ'3137
  • HY-N15686
    Torulene

    Torulin

    		 Apoptosis Androgen Receptor Bcl-2 Family MMP Cancer
    Torulene (Torulin) is an orally active carotenoid with anti-cancer activity. Torulene inhibits proliferation and induces apoptosis of tumor cells via a mitochondrial signal pathway and the down-regulation of androgen receptor (AR) expression. Torulene can be used for the study of prostate cancer .
    Torulene
  • HY-175652
    AZD9750

    		PROTACs Adenosine Receptor Cancer
    AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .
    AZD9750
  • HY-P10639
    C5aR2 agonist P32

    		Complement System Inflammation/Immunology
    C5aR2 agonist P32 (Ac-RHYPYWR-OH) is a C5aR2-selective agonist. C5aR2 agonist P32 has been shown to elicit multiple immunomodulatory activities, both by down-regulating the C5aR1-mediated cell signalling, and acting in a C5aR1-independent fashion, in vitro and in vivo .
    C5aR2 agonist P32
  • 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-N0138S1
    Theobromine-d3
    1 Publications Verification

    3,7-Dimethylxanthine-d3

    		 Adenosine Receptor Endogenous Metabolite Neurological Disease
    Theobromine-d3 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
    Theobromine-d3
  • HY-156084
    LL-K9-3

    		CDK PROTACs Apoptosis c-Myc Cancer
    LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .
    LL-K9-3
  • HY-117971
    BVT173187

    		CXCR Formyl Peptide Receptor (FPR) Others
    BVT173187 is a selective inhibitor of the neutrophil formyl peptide receptor FPR1, with activity that inhibits FPR1 activation. BVT173187 inhibits FPR1 agonist-induced activation in neutrophils, reduces adhesion molecule mobilization and superoxide anion production, and has inhibitory activity on FPR1 similar to that of earlier described peptide antagonists, but also has effects on C5aR and CXCR signaling.
    BVT173187
  • HY-N2673
    5-Heptadecylresorcinol

    5-n-Heptadecylresorcinol; AR-C17

    		 Sirtuin Cardiovascular Disease Metabolic Disease
    5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity .
    5-Heptadecylresorcinol
  • 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-179433
    PROTAC AR Degrader-12

    		PROTACs Androgen Receptor Estrogen Receptor/ERR Src Cancer
    PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
    PROTAC AR Degrader-12
  • HY-175231
    ST171

    		5-HT Receptor Neurological Disease
    ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research .
    ST171
  • HY-162325
    WJ-39

    		Aldose Reductase Mitochondrial Metabolism Apoptosis Mitophagy Metabolic Disease
    WJ-39 is an orally active aldose reductase (AR) inhibitor. WJ-39 improves tubular damage in diabetic nephropathy rats by activating PINK1/Parkin signaling, promoting mitophagy, and attenuating apoptosis .
    WJ-39
  • HY-N1731
    2′-Hydroxy-5′-methoxyacetophenone

    		NF-κB COX TNF Receptor NO Synthase Reactive Oxygen Species (ROS) Parasite Infection Metabolic Disease Inflammation/Immunology Cancer
    2'-Hydroxy-5'-methoxyacetophenone is an acetophenone derivative with acaricidal activities. 2'-Hydroxy-5'-methoxyacetophenone attenuates the inflammatory response via NF-κB signaling pathway. 2'-Hydroxy-5'-methoxyacetophenone exhibits significant inhibitory activity against α-amylase, collagenase and aldose reductase (AR) with IC50s of 0.928, 3.264 and 20.046 μM, highlighting its potential in combating diabetes. 2'-Hydroxy-5'-methoxyacetophenone exhibits anti-ovarian cancer activity .
    2′-Hydroxy-5′-methoxyacetophenone
  • HY-144127
    AR antagonist 3

    		Androgen Receptor Cancer
    AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
    AR antagonist 3
  • HY-N0138S
    Theobromine-d6

    3,7-Dimethylxanthine-d6

    		 Isotope-Labeled Compounds Adenosine Receptor Endogenous Metabolite Neurological Disease
    Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
    Theobromine-d6
  • HY-N0138R
    Theobromine (Standard)

    3,7-Dimethylxanthine (StandARd)

    		 Reference Standards Adenosine Receptor Endogenous Metabolite Neurological Disease
    Theobromine (Standard) is the analytical standard of Theobromine. This product is intended for research and analytical applications. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
    Theobromine (Standard)
  • HY-P11007
    β-catenin inhibitory peptoid

    		β-catenin Wnt Androgen Receptor Cancer
    β-catenin inhibitory peptoid (compound 13) inhibits the β-catenin:TCF interaction with an IC50 of 5.44 µM. β-catenin inhibitory peptoid inhibits both Wnt (IC50 of 0.105 µM) and androgen receptor (AR)-signaling (IC50 of 1.02 µM) in prostate cancer cell lines. β-catenin inhibitory peptoid markedly diminishes cell proliferation of prostate cancer cell lines .
    β-catenin inhibitory peptoid
  • HY-N2037R
    Higenamine (Standard)

    Norcoclaurine (StandARd); Demethyl-Coclaurine (StandARd)

    		 Reference Standards MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis Cardiovascular Disease Endocrinology
    Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
    Higenamine (Standard)
  • HY-N2673R
    5-Heptadecylresorcinol (Standard)

    5-n-Heptadecylresorcinol (StandARd); AR-C17 (StandARd)

    		 Reference Standards Sirtuin Cardiovascular Disease Metabolic Disease
    5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity .
    5-Heptadecylresorcinol (Standard)
  • HY-176225
    BY13

    		PROTACs Src Estrogen Receptor/ERR Apoptosis Cancer
    BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
    BY13
  • HY-P10639A
    C5aR2 agonist P32 acetate

    		Complement System Inflammation/Immunology
    C5aR2 agonist P32 (Ac-RHYPYWR-OH) acetate is a C5aR2-selective agonist. C5aR2 agonist P32 acetate has been shown to elicit multiple immunomodulatory activities, both by down-regulating the C5aR1-mediated cell signalling, and acting in a C5aR1-independent fashion, in vitro and in vivo .
    C5aR2 agonist P32 acetate
  • HY-119806
    TMPPAA

    		5-HT Receptor Neurological Disease
    TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .
    TMPPAA
  • HY-178148
    AR antagonist 17

    		Androgen Receptor Endocrinology Cancer
    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) .
    AR antagonist 17
  • HY-170948
    A2AR modulator-1

    		Adenosine Receptor Cancer
    A2AR modulator-1 (Compound 45) is a selective negative allosteric adenosine A2a receptor (A2aR) modulator with an IC50 value of 9 nM. A2AR modulator-1 reduces the affinity of endogenous adenosine for the receptor and inhibits cAMP signaling pathway activation. A2AR modulator-1 potently restores pCREB phosphorylation in CD4 + T cells, reversing immunosuppression in the tumor microenvironment, and shows potential to suppress tumor growth and metastasis in triple-negative breast cancer models .
    A2AR modulator-1
  • HY-136702
    L-97-1

    		Adenosine Receptor Inflammation/Immunology
    L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
    L-97-1
  • HY-173474
    ERβ agonist-1

    		Estrogen Receptor/ERR Androgen Receptor Cancer
    ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
    ERβ agonist-1
  • HY-105122
    Zanoterone

    WIN 49596

    		 Androgen Receptor Endocrinology Cancer
    Zanoterone is an orally active antagonist of the androgen receptor (AR) with a Ki of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .
    Zanoterone
  • HY-N3716
    Dehydroglyasperin D

    		Aldose Reductase COX Metabolic Disease Inflammation/Immunology
    Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC50: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi .
    Dehydroglyasperin D
  • HY-N7043R
    Isosilybin A (Standard)

    		Reference Standards Apoptosis PPAR NF-κB p38 MAPK ERK Androgen Receptor Inflammation/Immunology Cancer
    Isosilybin A (Standard) is the analytical standard of Isosilybin A (HY-N7043). Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity [1][2][3].
    Isosilybin A (Standard)
  • HY-N2908R
    Atraric acid (Standard)

    Methyl atrARate (StandARd)

    		 Reference Standards Androgen Receptor NO Synthase p38 MAPK NF-κB Inflammation/Immunology Cancer
    Atraric acid (Standard) is the analytical standard of Atraric acid. This product is intended for research and analytical applications. Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2].
    Atraric acid (Standard)
  • HY-N0819R
    Raddeanin A (Standard)

    		Reference Standards Apoptosis PI3K Akt ERK mTOR Wnt β-catenin Wee1 JNK VEGFR CDK Neurological Disease Inflammation/Immunology Cancer
    Raddeanin A (Standard) is the analytical standard of Raddeanin A (HY-N0819). This product is intended for research and analytical applications. Raddeanin A is an oleanane-type triterpenoid saponin with oral activity. Raddeanin A inhibits SRC, mTOR, JNK, VEGFR2, NLRP3 inflammasome, Wnt/β-catenin, Wee1, PI3K/AKT signaling pathway, MAPK/ERK signaling pathway, AR-FL, AR-Vs, and downregulates the expression of p-PI3K and p-AKT. Raddeanin A inhibits osteoclast formation, bone resorption, osteolysis, cancer cell invasion, migration, proliferation, angiogenesis and epithelial-mesenchymal transition, while induces apoptosis, cell cycle arrest, ROS production, immunogenic cell death and dendritic cell maturation. Raddeanin A improves blood-retinal barrier function, alleviates inflammation, regulates the tumor microenvironment, and enhances the activity of anti-PD-1 antibody. Raddeanin A is applicable to the research of breast cancer-associated osteolysis, human osteosarcoma, colorectal cancer, glioblastoma, Alzheimer's disease, cholangiocarcinoma, melanoma, non-small cell lung cancer, castration-resistant prostate cancer and multiple myeloma.
    Raddeanin A (Standard)
  • HY-111024R
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard)

    PMC (StandARd)

    		 Reference Standards Androgen Receptor NF-κB Cardiovascular Disease Inflammation/Immunology Cancer
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard) is the analytical standard of 2,2,5,7,8-Pentamethyl-6-Chromanol. This product is intended for research and analytical applications. 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines[1].
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard)
  • HY-183667
    JNJ-pan-AR

    		Androgen Receptor Kallikrein Cancer
    JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer .
    JNJ-pan-AR

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