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Results for "

AR-FL

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148771
    MTX-23

    PROTAC AR-V7 degrader-2

    		 PROTACs Androgen Receptor Apoptosis Cancer
    MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis .
    MTX-23
  • HY-400766
    BWA-522 intermediate-2

    		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-W877989
    BWA-522 intermediate-1

    		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-164373
    SC428

    		Androgen Receptor Apoptosis Cancer
    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 .
    SC428
  • HY-149433
    BWA-522

    		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-161409
    SC912

    		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-153918
    (R)-SKBG-1

    		Androgen Receptor Cancer
    (R)-SKBG-1 is a covalent inhibitor targeting the RNA binding protein NONO. (R)-SKBG-1 can reduce the expression of androgen receptor (AR) and its splice variants, inhibiting cancer cell proliferation. (R)-SKBG-1 inhibits androgen receptor expression with IC50 of 3.1 μM and 5.5 μM for AR-FL mRNA and AR-V7 mRNA, respectively. (R)-SKBG-1 interferes with the gene regulatory network of cancer cells and inhibits cancer cell growth by stabilizing the interaction between NONO and mRNA. (R)-SKBG-1 can be used in the study of cancers related to NONO dysfunction, such as prostate cancer .
    (R)-SKBG-1
  • HY-150102
    EPI-7170

    		Androgen Receptor Cancer
    EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
    EPI-7170
  • HY-170329
    PROTAC AR Degrader-8

    		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-401056
    BWA-522 intermediate-3

    		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-124628
    IPI-9119
    1 Publications Verification

    		 Fatty Acid Synthase (FASN) Cancer
    IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
    IPI-9119

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