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castration-resistant prostate cancer cells

" in MedChemExpress (MCE) Product Catalog:

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9

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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-P3371
    Ifinatamab deruxtecan

    DS-7300a; MABX-9001a; I-DXd

    		 Antibody-Drug Conjugates (ADCs) Topoisomerase Apoptosis Cancer
    Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
    Ifinatamab deruxtecan
  • HY-P991015
    Pasritamig

    JNJ-78278343; KLCB-245

    		 CD3 Cancer
    Pasritamig (JNJ-78278343; KLCB-245) is a bispecific T-cell engager (BiTE) that targets the complex of human kallikrein KLK2 and CD3 receptor. Pasritamig redirects the cytotoxicity of T cells to KLK2-expressing tumor cells and induces T cell-mediated lysis of KLK2-expressing prostate cancer cells. Administered via subcutaneous injection, subcutaneous infusion or intravenous infusion, Pasritamig exhibits antitumor activity against metastatic castration-resistant prostate cancer. Pasritamig has a safety profile with an extremely low incidence of cytokine release syndrome and can be safely administered in an outpatient setting. Pasritamig is applicable to the research of metastatic castration-resistant prostate cancer .
    Pasritamig
  • HY-P990688
    Xaluritamig

    AMG-509

    		 CD3 Cancer
    Xaluritamig (AMG-509) is a bispecific T cell engager and cytolytic agent with a Kd of 27.6 nM for human CD3ε. Xaluritamig binds to CD3ε via an anti-CD3 single-chain variable fragment (scFv) domain, and to STEAP1 via a bispecific anti-STEAP1 antigen-binding fragment (Fab) domain, thereby recruiting and activating T cells and forming a bridge between T cells and STEAP1-expressing cancer cells. Xaluritamig induces T cell-mediated redirected cytotoxicity, tumor cell lysis, cytokine release, CD8 + T cell activation and expansion, as well as tumor stasis or regression. Xaluritamig contains an Fc domain with no effector function, which prolongs serum half-life, exhibits only minimal activity against cells with low STEAP1 expression and normal cells, and shows extremely low target-related off-tumor toxicity in cynomolgus monkeys. Xaluritamig is used in STEAP1×CD3 XmAb 2+1 immunotherapy and in research on metastatic castration-resistant prostate cancer and Ewing sarcoma .
    Xaluritamig
  • HY-P990673
    Vandortuzumab

    DSTP-3086S Antibody; RG-7450 Antibody

    		 ADC Antibody Transmembrane Glycoprotein Mitosis Cancer
    Vandortuzumab (DSTP-3086S Antibody; RG-7450 Antibody) is a humanized anti-STEAP1 IgG1 antibody and antimitotic agent that can be conjugated with MMAE (HY-15162) to form the antibody-drug conjugate (ADC) Vandortuzumab vedotin. Vandortuzumab vedotin specifically binds to STEAP1 and drives internalization of the complex, releasing the MMAE (HY-15162) payload intracellularly. After binding to tubulin, MMAE inhibits cell division and induces cell death. Vandortuzumab exhibits antitumor activity in preclinical xenograft models of prostate cancer and can be used for research related to metastatic castration-resistant prostate cancer (mCRPC) .
    Vandortuzumab
  • HY-112078
    (S,R,S)-AHPC-Me

    VHL ligand 2; E3 ligase Ligand 1A

    		 Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me
  • HY-N6796
    Manumycin A
    2 Publications Verification

    		 Antibiotic Exosomes Farnesyl Transferase Ras Apoptosis Phospholipase TNF Receptor Atg8/LC3 Infection Inflammation/Immunology Cancer
    Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
    Manumycin A
  • HY-P99802
    Pasotuxizumab
    1 Publications Verification

    BAY 2010112; AMG 212; MT112

    		 CD3 Cancer
    Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
    Pasotuxizumab
  • HY-42424
    (S,R,S)-AHPC-Me hydrochloride

    VHL ligand 2 hydrochloride; E3 ligase Ligand 1

    		 Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me hydrochloride
  • HY-70006
    Galeterone
    3 Publications Verification

    TOK-001; VN-124-1

    		 Molecular Glues Androgen Receptor MNK Cytochrome P450 Apoptosis Cancer
    Galeterone (TOK-001) is a potent, 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. Galeterone also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research [1][2].
    Galeterone
  • HY-N5074
    Terrestrosin D

    		Apoptosis VEGFR Inflammation/Immunology Cancer
    Terrestrosin D is an orally active apoptosis inducer. Terrestrosin D induces cell cycle arrest at the G1 and S phases, reduces mitochondrial membrane potential, and inhibits the growth of cancer cells and endothelial cells. Terrestrosin D is studied in castration-resistant prostate cancer and pulmonary fibrosis .
    Terrestrosin D
  • HY-P9992
    Pelgifatamab

    BAY-2315497; PSMA-TTC

    		 PSMA Apoptosis Cancer
    Peligifatamab is a PSMA-targeted α-radioimmunoconjugate with an EC50 of 1.2 nM against human targets. Peligifatamab induces DNA damage, DNA double-strand breaks, cell cycle arrest and apoptosis (Apoptosis) in PSMA-positive prostate cancer cells. Peligifatamab reduces cell viability in a manner dependent on cellular PSMA expression levels. Peligifatamab inhibits tumor growth and tumor-induced abnormal bone growth in prostate cancer bone metastasis models. Peligifatamab exhibits antitumor efficacy in subcutaneous prostate cancer models and xenograft models. Peligifatamab can be used for the research of metastatic castration-resistant prostate cancer .
    Pelgifatamab
  • HY-145722
    Apatorsen sodium
    1 Publications Verification

    OGX-427 sodium

    		 HSP Cancer
    Apatorsen (OGX-427) sodium is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen sodium reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen sodium is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer .
    Apatorsen sodium
  • HY-15194
    Dimethylcurcumin
    Maximum Cited Publications
    14 Publications Verification

    ASC-J9; GO-Y025

    		 Androgen Receptor Cancer
    Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
    Dimethylcurcumin
  • HY-45661
    Inixaciclib

    NUV-422

    		 CDK Neurological Disease Cancer
    Inixaciclib (NUV-422) is a blood-brain barrier-penetrant inhibitor of CDK2, CDK4 and CDK6. Inixaciclib inhibits cancer cell growth. Inixaciclib induces anti-tumor activity in xenograft models of glioblastoma, CDK4/CDK6 inhibitor-resistant HR + HER2 - metastatic breast cancer, and anti-androgen-resistant prostate cancer. Inixaciclib can be used for the research of relapsed or metastatic castration-resistant prostate cancer .
    Inixaciclib
  • 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-19337
    Ketodarolutamide
    1 Publications Verification

    BAY 1896953; ORM-15341

    		 Androgen Receptor Cancer
    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 .
    Ketodarolutamide
  • HY-134635
    Dehydrozingerone

    		Bacterial Fungal HIV CDK Infection Cancer
    Dehydrozingerone is a ginger-derived component and cyclin D1 inhibitor that downregulates cyclin D1 expression and induces cell cycle G1 phase arrest. Dehydrozingerone reduces the proliferative capacity of castration-resistant prostate cancer cells under in vitro conditions. Dehydrozingerone reduces subcutaneous tumor growth by inhibiting cell proliferation and angiogenesis. Dehydrozingerone exerts antibacterial and antifungal activities via its α,β-unsaturated carbonyl conjugated system. Dehydrozingerone can be used in studies related to castration-resistant prostate cancer, bacterial infections, and food spoilage fungal infections .
    Dehydrozingerone
  • 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-P99217
    Rilotumumab

    AMG 102

    		 c-Met/HGFR Cancer
    Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
    Rilotumumab
  • HY-170329
    PROTAC AR Degrader-8

    		PROTACs Androgen Receptor Apoptosis Cancer
    PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s 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 values 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. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer .
    PROTAC AR Degrader-8
  • HY-P99714
    Lorigerlimab

    MGD019

    		 PD-1/PD-L1 CTLA-4 Cancer
    Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
    Lorigerlimab
  • HY-115282A
    JNJ-63576253
    1 Publications Verification

    TRC-253

    		 Androgen Receptor Cancer
    JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
    JNJ-63576253
  • HY-145722A
    Apatorsen
    1 Publications Verification

    OGX-427

    		 HSP Cancer
    Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer .
    Apatorsen
  • HY-149894
    MC-1-F2

    		c-Myc Cadherin Cancer
    MC-1-F2 is a FOXC2 inhibitor. MC-1-F2 shows a binding affinity (Kd) of 26 μM for full-length FOXC2. MC-1-F2 reduces epithelial-mesenchymal transition (EMT) markers in breast cancer cells, suppresses cancer stem cell (CSC) properties and reduces invasiveness in castration-resistant prostate cancer (CRPC) cells. MC-1-F2 can be used for the study of CRPC and breast cancer .
    MC-1-F2
  • HY-160777
    VNPP433-3β

    Galeterone 3β-imidazole

    		 Molecular Glues Androgen Receptor MNK Apoptosis Cancer
    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 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-42424A
    (S,R,S)-AHPC-Me dihydrochloride

    VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    		 Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me dihydrochloride
  • HY-160187A
    (Rac)-AAA

    		Cadherin MMP Akt FAK ERK NF-κB Cancer
    (Rac)-AAA is a regulator and inhibitor targeting GPR75. By blocking the 20-HETE-induced downregulation of GPR75 expression, (Rac)-AAA effectively inhibits the activation of key downstream signaling pathways including EGFR, AKT, NF-κB and FAK. (Rac)-AAA reverses 20-HETE-mediated epithelial-mesenchymal transition, which is specifically characterized by downregulating vimentin (vimentin), upregulating E-Cadherin, as well as reducing MMP-2 activity and cancer cell migration ability. (Rac)-AAA also abolishes the 20-HETE-induced upregulation of HIC-5 expression and anchorage-independent growth, and modulates the subcellular localization of PKC-α and phosphorylated AKT. (Rac)-AAA is investigated in androgen-independent prostate cancer (castration-resistant prostate cancer) .
    (Rac)-AAA
  • 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-144636
    Atg4B-IN-2

    		Atg4 Cathepsin Phospholipase Autophagy Cancer
    Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
    Atg4B-IN-2
  • 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-175455
    LYA914

    		PROTACs Androgen Receptor Akt Cancer
    LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .
    LYA914
  • 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-179056
    Psa-AR

    		PROTACs PSMA Androgen Receptor HSP Apoptosis Cancer
    Psa-AR is a PROTAC degrader targeting PSMA, with a Kd of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer .
    Psa-AR
  • HY-70006A
    Galeterone hydrochloride

    TOK-001 hydrochloride; VN-124-1 hydrochloride

    		 Molecular Glues Androgen Receptor MNK Cytochrome P450 Apoptosis Cancer
    Galeterone (TOK-001) hydrochloride is a potent, 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. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research [1][2].
    Galeterone hydrochloride
  • HY-173186
    TLK1-IN-1

    		TLK Apoptosis Cancer
    TLK1-IN-1 is a TLK1B inhibitor with a human IC50 of 7.2 μM. TLK1-IN-1 causes accumulation of DNA damage and induces apoptotic cell death in cancer cells. TLK1-IN-1 can be used for the research of metastatic castration-resistant prostate cancer .
    TLK1-IN-1
  • HY-P10743
    BQ7876

    		Radionuclide-Drug Conjugates (RDCs) PSMA Cancer
    BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumor cell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC) . BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    BQ7876
  • HY-174908
    SJL2-1

    		Histone Methyltransferase 11β-HSD Androgen Receptor Cancer
    SJL2-1 is a PRMT5 inhibitor, with an IC50 of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC) .
    SJL2-1
  • HY-153718
    KI-ARv-03

    		Ligands for Target Protein for PROTAC CDK c-Myc Cancer
    KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32 (HY-173523) [1][2].
    KI-ARv-03
  • HY-170820
    XYD049

    		Molecular Glues Bcl-2 Family CDK EGFR HSP Androgen Receptor c-Myc Cancer
    XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC50 of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
    XYD049
  • HY-141830
    SYY-B029-2

    		Histone Acetyltransferase Cancer
    SYY-B029-2 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 of 1.4 nM. SYY-B029-2 cell growth of human mantle cell lymphoma (MCL) cell line MAVER-1 and human castration resistant prostate cancer cell line LNCaP clone FGC, with IC50 values of 15 nM and 13 nM, respectively .
    SYY-B029-2
  • HY-178938
    AR Degrader-3

    		Molecular Glues Androgen Receptor Caspase Apoptosis Endocrinology Cancer
    AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC) .
    AR Degrader-3
  • HY-113701
    CH5137291

    		Androgen Receptor Cancer
    CH5137291 is an orally active pure antagonist of the androgen receptor (AR), without generating agonist metabolites. CCH5137291 directly blocks the transfer of AR from the cytoplasm to the nucleus. H5137291 can completely inhibit tumor growth in cells and mouse models of castration-resistant prostate cancer models. CH5137291 can be used for the study of castration-resistant prostate cancer (CRPC) .
    CH5137291
  • HY-160777A
    VNPP433-3β dihydrochloride

    Galeterone 3β-imidazole dihydrochloride

    		 Molecular Glues Androgen Receptor MNK Apoptosis Cancer
    VNPP433-3β (Galeterone 3β-imidazole) dihydrochloride 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 dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
    VNPP433-3β dihydrochloride
  • HY-160777B
    VNPP433-3β hydrochloride

    Galeterone 3β-imidazole hydrochloride

    		 Molecular Glues Androgen Receptor MNK Apoptosis Cancer
    VNPP433-3β (Galeterone 3β-imidazole) hydrochloride 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 hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
    VNPP433-3β hydrochloride
  • HY-152512
    RLA-4842

    		Androgen Receptor Cancer
    RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
    RLA-4842
  • HY-152520
    RLA-5331

    		Androgen Receptor Cancer
    RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
    RLA-5331
  • HY-163192
    W6134

    		ROR Apoptosis Cancer
    W6134 is highly potent and selective RORγ covalent inhibitor with an IC50 of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC) .
    W6134
  • 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-173273
    YJZ5118

    		CDK Apoptosis DNA/RNA Synthesis Akt Cancer
    YJZ5118 is a selective CDK12/CDK13 inhibitor with IC50 values of 39.5 nM and 26.4 nM. YJZ5118 suppresses transcription of DNA damage response genes and induces DNA damage in tumor cells. YJZ5118 inhibits proliferation and triggers apoptosis. YJZ5118 inhibits RNA polymerase II Ser2 phosphorylation and increases Akt pathway activity. YJZ5118 exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for the research of cancer, such as prostate cancer .
    YJZ5118

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