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AR protein

" in MedChemExpress (MCE) Product Catalog:

82

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4

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19

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111848A

    SNIPERs PROTACs Androgen Receptor Cancer
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
    PROTAC AR Degrader-4 TFA
  • HY-160262

    Androgen Receptor PROTACs Epigenetic Reader Domain Cancer
    AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research .
    AR/BET protein degrader-1
  • HY-173373

    Ligands for Target Protein for PROTAC Androgen Receptor Cancer
    AR ligand-39, an orally active and selective androgen receptor (AR) antagonist, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). AR ligand-39 can be used for synthesis PROTAC AR Degrader-10 (HY-173372) .
    AR ligand-39
  • HY-149434

    Androgen Receptor Apoptosis Cancer
    PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .
    PROTAC AR-NTD degrader 1
  • HY-176129

    Ligands for Target Protein for PROTAC Cancer
    AR ligand 41 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). AR ligand 41 can be used for the synthesis of BWA-6047 (HY-176128) .
    AR ligand 41
  • HY-170303

    Ligands for Target Protein for PROTAC Cancer
    AR ligand-32 is a target protein ligand, used for the synthesis of PROTAC AR Degrader-7 (HY-160221) .
    AR ligand-32
  • HY-174391

    Androgen Receptor Apoptosis Cancer
    AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer.
    AR antagonist 15
  • HY-169967

    Ligands for Target Protein for PROTAC Cancer
    AR ligand-31 is a PROTAC target protein ligand that can be used to synthesize PROTAC AR Degrader-5 (HY-160547) .
    AR ligand-31
  • HY-111848

    SNIPERs PROTACs Androgen Receptor Cancer
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
    PROTAC AR Degrader-4
  • HY-173372

    Androgen Receptor Cancer
    PROTAC AR Degrader-10 is a protein degrader targeting the androgen receptor (AR) with a DC50 value ≤100 nM. PROTAC AR Degrader-10 can be used for prostate cancer study. (Structure Note: Pink: target protein ligand (HY-173373); Blue: E3 ligase ligand (HY-138793); Black: linker) .
    PROTAC AR Degrader-10
  • HY-170330

    Ligands for Target Protein for PROTAC Androgen Receptor Cancer
    AR ligand-33 is the ligand for androgen receptor, that can be used for synthesis of PROTAC AR Degrader-8 (HY-170329) as the target protein ligand .
    AR ligand-33
  • HY-173559

    Androgen Receptor Cancer
    AR antagonist 12 (compound 20i) is an orally active androgen receptor antagonist wiith IC50 values of 119.3 μM and 98.2 μM for wt-AR and AR-F877L,respectively. AR antagonist 12 induces a dose-dependent and time-dependent reduction in AR, AR-V7, and PSA protein levels. AR antagonist 1 shows anticancer activuty and can be used for the study of Enzalutamide (HY-70002)-resistant Prostate cancer .
    AR antagonist 12
  • HY-173409

    Androgen Receptor Ser/Thr Protease Inflammation/Immunology
    AR antagonist 11 (Compound c2) is a selective AR antagonist with an IC50 of 0.019 μM. AR antagonist 11 is also effective against AR F877L/T878A mutant (IC50: 1.03 μM). AR antagonist 11 inhibits LNCaP cell proliferation and reduces PSA protein expression (IC50: 0.54 μM). AR antagonist 11 can be used for research of prostate cancer (PCa) .
    AR antagonist 11
  • HY-174157

    Autophagy AMPK Neurological Disease Metabolic Disease
    AR493 is an autophagy activator acting on AMPK (adenosine monophosphate-activated protein kinase). AR493 regulates pathways related to cellular energy sensing and increases autophagy levels. AR493 is promising for research of aging-associated diseases (such as diabetes, neurodegenerative diseases) and autophagy regulation .
    AR493
  • HY-176067

    Androgen Receptor Cancer
    LO-4-25 is a covalent degrader targeting the androgen receptor (AR) and its truncated variant AR-V7. LO-4-25 covalently binds to the E3 ubiquitin ligase CUL4 DCAF16, promoting the ubiquitination of AR and AR-V7, which subsequently are recognized and degraded by the proteasome, reducing the protein levels of AR and AR-V7 in cells. LO-4-25 is promising for research of androgen-independent prostate cancers .
    LO-4-25
  • HY-172624

    Ligands for Target Protein for PROTAC Cancer
    AR antagonist 14 is is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). AR antagonist 14 can be combined with VH 101-amide-piperidine-Pip-alkyne (HY-172625) to synthesize PROTAC degraders (ARD-69 (HY-114402)) .
    AR antagonist 14
  • HY-150025

    DNA Methyltransferase Apoptosis Cancer
    (4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 .
    (4aS,8aR)-NPD-001
  • HY-W653723

    NDCHA

    Androgen Receptor Endocrinology
    N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
    N-Nitrosodicyclohexylamine
  • HY-130845

    Ligands for E3 Ligase Ligands for Target Protein for PROTAC Cancer
    AR antagonist 1 (compound 29) 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
  • HY-130992

    Androgen Receptor Ligands for Target Protein for PROTAC Cancer
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .
    Androgen receptor antagonist 1
  • HY-132292

    PROTACs Androgen Receptor Cancer
    ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .
    ARD-2128
  • HY-164552

    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-130845A

    Ligands for E3 Ligase Ligands for Target Protein for PROTAC Androgen Receptor Cancer
    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-400766

    Drug Intermediate Cancer
    BWA-522 intermediate-2 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
    BWA-522 intermediate-2
  • HY-401056

    Drug Intermediate Cancer
    BWA-522 intermediate-3 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
    BWA-522 intermediate-3
  • HY-121588

    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-148777

    PROTACs Androgen Receptor Cancer
    A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP) .
    A031
  • HY-110202

    Adenosine Receptor Neurological Disease Inflammation/Immunology
    MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis .
    MRS5698
  • HY-160547

    PROTACs Androgen Receptor Metabolic Disease
    PROTAC AR Degrader-5 (compound A46) is a potent AR PROTACs degrader with an IC50 value of 49 nM. PROTAC AR Degrader-5 inhibits sebaceous plaque and induces hair regeneration (Pink: ligand for target protein (HY-169967); black: linker (HY-169966); Blue: E3 ligase ligand (HY-125845)) .
    PROTAC AR Degrader-5
  • HY-161409

    Androgen Receptor Apoptosis Cancer
    SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .
    SC912
  • HY-168697

    Ligands for Target Protein for PROTAC Cancer
    AR ligand-37 is a PROTAC target protein ligand that can be used to synthesize BMS-986365 (HY-158101) .
    AR ligand-37
  • HY-149433

    Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
    BWA-522
  • HY-168299

    Androgen Receptor Ligands for Target Protein for PROTAC Cancer
    AR ligand-30 is a target protein ligand for PROTAC Bavdegalutamide (HY-138641), which can be used in prostate cancer research .
    AR ligand-30
  • HY-W653723R

    NDCHA (StandARd)

    Reference Standards Androgen Receptor Endocrinology
    N-Nitrosodicyclohexylamine (Standard) is the analytical standard of N-Nitrosodicyclohexylamine. This product is intended for research and analytical applications. N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
    N-Nitrosodicyclohexylamine (Standard)
  • HY-133045

    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-170448

    PROTACs Androgen Receptor Endocrinology
    PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models . (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))
    PROTAC AR Degrader-9
  • HY-19319

    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-149862

    PROTACs Androgen Receptor Cancer
    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-B1421

    LY031537

    Adrenergic Receptor Metabolic Disease
    Ractopamine (LY031537) hydrochloride is a potent β-adrenergic receptor (βAR) agonist with Kd value of ~25 nM for pig β1AR and β2AR. Ractopamine hydrochloride is linked to protein metabolism. Ractopamine hydrochloride can be used for researching to increase lean tissue growth and improve production efficiency in pigs .
    Ractopamine hydrochloride
  • 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-168296

    Ligands for Target Protein for PROTAC Cancer
    AR ligand-29 is the target protein ligand of PROTAC VinclozolinM2-2204 (HY-161741), which can be used for cancer research .
    AR ligand-29
  • HY-170329

    PROTACs Androgen Receptor Apoptosis Cancer
    PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model . (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))
    PROTAC AR Degrader-8
  • HY-158882

    Biochemical Assay Reagents Adenosine Receptor Others
    FLAC6 is a potent fluorinated detergent that can be used to solubilize membrane proteins (the native adenosine receptor A2AR, a G protein-coupled receptor, and two native transporters AcrB and BmrA). FLAC6 can maintain the structural and functional integrity of different membrane proteins .
    FLAC6
  • HY-114402

    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 the treatment 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-169385

    AUTOTACs Androgen Receptor Cancer
    ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa . ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
    ATC-324
  • HY-W877989

    Ligands for E3 Ligase Cancer
    BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7 .
    BWA-522 intermediate-1
  • HY-148361

    FAP Others
    Fluorogen binding modulator-1 (PubChem SID 125240934) is a fluorogen activating protein (FAP)-fluorogen binding modulator with -log EC50s of 6.61 and 6.37 for AM2.2-β2AR and AM2.2-GPR32, respectively .
    Fluorogen binding modulator-1
  • HY-124292
    Honokiol DCA
    1 Publications Verification

    Honokiol dichloroacetate

    Androgen Receptor Cancer
    Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level .
    Honokiol DCA
  • HY-133020

    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-157491

    PROTACs Androgen Receptor Epigenetic Reader Domain Cancer
    K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells .
    K2-B4-5e

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