Search Result
Results for "
CRPC
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-149894
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Biochemical Assay Reagents
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Cancer
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MC-1-F2 is a FOXC2 inhibitor that 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. There is a synergistic effect between MC-1-F2 and Docetaxel, which has the potential to be used in combination to study CRPC .
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- HY-10088
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ZD4054
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Endothelin Receptor
Apoptosis
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Endocrinology
Cancer
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Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
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- HY-114902
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Epigenetic Reader Domain
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Cancer
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Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research .
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- HY-161023
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Others
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Cancer
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Importin β1-IN-1 (compound DD1-Br) is an orally active Importin β1 inhibitor (KD = 0.219 μM). Importin β1-IN-1 exhibits antiproliferative activity on castration-resistant prostate cancer (CRPC) cells. Importin β1-IN-1 alone or in combination with enzalutamide completely prevented tumor growth in a mouse model of drug-resistant CRPC. Importin β1-IN-1 can be used in cancer research .
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- HY-161287
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HDAC
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Cancer
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HDAC6-IN-32 (compound 25202) is a selective and potent inhibitor of HDAC6. HDAC6-IN-32 blocks HDAC6 activity and interferes with microtubule dynamics, leading to SAC activation and prolonged mitotic arrest, ultimately leading to apoptosis in CRPC cells .
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- HY-137193
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Drug Metabolite
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Cancer
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5,6-Dihydroabiraterone is the metabolism of Abiraterone (HY-70013). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, and shows antitumor activity in CRPC (castration-resistant prostate cancer) .
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- HY-139104
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DNA/RNA Synthesis
Apoptosis
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Cancer
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Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis .
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- HY-P99217
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AMG 102
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c-Met/HGFR
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Cancer
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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 .
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- HY-109070
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EPI-002
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Androgen Receptor
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Cancer
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Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-115282A
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TRC-253
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Androgen Receptor
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Cancer
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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) .
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- HY-138557
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17β-HSD
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Cancer
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AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research .
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- HY-115282
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TRC-253 free base
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Androgen Receptor
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Cancer
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JNJ-63576253 (TRC-253) free base 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 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-124628
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Fatty Acid Synthase (FASN)
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Cancer
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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 .
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- HY-145388
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PROTACs
Epigenetic Reader Domain
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Cancer
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AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
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- HY-10617D
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AG014699 acetate; PF-01367338 acetate
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PARP
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Cancer
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Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-10617B
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AG014699 hydrochloride; PF-01367338 hydrochloride
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PARP
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Cancer
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Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-150102
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Androgen Receptor
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Cancer
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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) .
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- HY-10617C
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AG-014699 tartrate; PF-01367338 tartrate
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PARP
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Cancer
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Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-N0790
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Lupeol
3 Publications Verification
Clerodol; Monogynol B; Fagarasterol
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Androgen Receptor
Apoptosis
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Cancer
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Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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- HY-70006
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TOK-001; VN-124-1
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Cytochrome P450
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Cancer
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Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
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- HY-111503
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Epigenetic Reader Domain
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Cancer
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Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM .
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- HY-137448
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SHR3680
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Androgen Receptor
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Cancer
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Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer .
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- HY-139970
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Androgen Receptor
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Endocrinology
Cancer
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VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
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- HY-10617
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AG-014699 phosphate; PF-01367338 phosphate
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PARP
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Cancer
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Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-10617A
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Rucaparib
Maximum Cited Publications
33 Publications Verification
AG014699; PF-01367338
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PARP
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Cancer
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Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-102003
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AG014699 monocamsylate; PF-01367338 monocamsylate
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PARP
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Cancer
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Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-102003A
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AG014699 camsylate; PF-01367338 camsylate
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PARP
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Cancer
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Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-161700
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Cytochrome P450
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Cancer
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BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels .
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- HY-19319
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Epigenetic Reader Domain
Androgen Receptor
Apoptosis
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Cancer
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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 .
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- HY-163192
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ROR
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Cancer
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W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM. W6134 exhibits superior activity ini nhibiting the proliferation and colony formation and inducing apoptosis. W6134 can be used for the research of cancer .
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- HY-121522
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Histone Demethylase
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Cancer
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SD-70 is an inhibitor for histone demethylase JMJD2C and exhibits antitumor efficacy. SD-70 inhibits viability of cancer cells CWR22Rv1 (9% cell survival at 10 μM), PC3 (14% cell survival at 2 μM) and DU145 (26% cell survival at 2 μM) .
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- HY-42424
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VHL ligand 2 hydrochloride; E3 ligase Ligand 1
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Ligands for E3 Ligase
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Cancer
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(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 .
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- HY-112078
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VHL ligand 2; E3 ligase Ligand 1A
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Ligands for E3 Ligase
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Cancer
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(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 .
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- HY-42424A
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VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
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Ligands for E3 Ligase
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Cancer
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(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 .
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- HY-137478A
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CDK
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Cancer
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KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity .
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- HY-137478
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CDK
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Cancer
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KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity .
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- HY-135794
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11-KDHT; 5α-Dihydro-11-keto testosterone
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Androgen Receptor
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Endocrinology
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11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells .
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- HY-160777
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Galeterone 3β-imidazole
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Androgen Receptor
MNK
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Cancer
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VNPP433-3β is a 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 inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99217
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AMG 102
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c-Met/HGFR
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Cancer
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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 .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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