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Results for "

castrated

" in MedChemExpress (MCE) Product Catalog:

By Targets:	17β-HSD (1) ADC Linker (2) Androgen Receptor (16) Apoptosis (4) Atg4 (1) Autophagy (1) Biochemical Assay Reagents (1) c-Met/HGFR (1) Cathepsin (1) CD3 (1) CTLA-4 (1) Cytochrome P450 (1) DNA Alkylator/Crosslinker (1) DNA-PK (2) Drug Metabolite (1) Endothelin Receptor (1) Epigenetic Reader Domain (4) Fatty Acid Synthase (FASN) (1) Glucocorticoid Receptor (1) GnRH Receptor (2) HDAC (2) Isotope-Labeled Compounds (1) Ligands for E3 Ligase (3) PARP (7) PD-1/PD-L1 (1) PERK (1) Phospholipase (1) PPAR (1) PROTACs (2) PSMA (3) STAT (1)
By Research Areas:	Cancer (53) Endocrinology (3) Metabolic Disease (1)

By Targets:

17β-HSD (1)

ADC Linker (2)

Androgen Receptor (16)

Apoptosis (4)

Atg4 (1)

Autophagy (1)

Biochemical Assay Reagents (1)

c-Met/HGFR (1)

Cathepsin (1)

CD3 (1)

CTLA-4 (1)

Cytochrome P450 (1)

DNA Alkylator/Crosslinker (1)

DNA-PK (2)

Drug Metabolite (1)

Endothelin Receptor (1)

Epigenetic Reader Domain (4)

Fatty Acid Synthase (FASN) (1)

Glucocorticoid Receptor (1)

GnRH Receptor (2)

HDAC (2)

Isotope-Labeled Compounds (1)

Ligands for E3 Ligase (3)

PARP (7)

PD-1/PD-L1 (1)

PERK (1)

Phospholipase (1)

PPAR (1)

PROTACs (2)

PSMA (3)

STAT (1)

By Research Areas:

Cancer (53)

Endocrinology (3)

Metabolic Disease (1)

Inhibitors & Agonists

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19319

MI-136	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 K_d of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors .

HY-111145

RD162	Androgen Receptor	Cancer
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .

HY-13699

NBI-42902	GnRH Receptor PERK	Others
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC₅₀ value of 0.79 nM, a K_i value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca ²⁺ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .

HY-109070

Ralaniten EPI-002	Androgen Receptor	Cancer
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) .

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) .

HY-138557

AKR1C3-IN-4	17β-HSD	Cancer
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 .

HY-115282

JNJ-63576253 free base TRC-253 free base	Androgen Receptor	Cancer
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) .

HY-112257

S-23 1 Publications Verification	Androgen Receptor	Metabolic Disease
S-23 is an orally active selective androgen receptor modulator (SARM) with a K_i of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats .

HY-N0790

Lupeol 3 Publications Verification Clerodol; Monogynol B; Fagarasterol	Androgen Receptor Apoptosis	Cancer
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) .

HY-143535

HG122

Androgen Receptor Cancer

HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.

HG122	Androgen Receptor	Cancer
HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.

HY-70006

Galeterone 2 Publications Verification TOK-001; VN-124-1	Cytochrome P450	Cancer
Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC₅₀=47 nM) in castration resistant prostate cancer (CRPC).

HY-15194

Dimethylcurcumin 10+ Cited Publications 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.

HY-111503

Y06137	Epigenetic Reader Domain	Cancer
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 K_d of 81 nM .

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 .

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 .

HY-149927

Antitumor agent-91	Others	Cancer
Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .

HY-128938

EC1167	ADC Linker	Cancer
EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC) .

HY-125170

Galiellalactone	STAT	Cancer
Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC₅₀ of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer .

HY-128938A

EC1167 hydrochloride	ADC Linker	Cancer
EC1167 hydrochloride is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 hydrochloride has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC) .

HY-137193

5,6-Dihydroabiraterone	Drug Metabolite	Cancer
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) .

HY-10088

Zibotentan ZD4054	Endothelin Receptor Apoptosis	Endocrinology Cancer
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ET_A) receptor antagonist with a K_i 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 .

HY-124628

IPI-9119	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 .

HY-146397

TD-802	PROTACs Androgen Receptor	Cancer
TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .

HY-10528

Tasquinimod 5+ Cited Publications ABR-215050	HDAC	Cancer
Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn ²⁺ binding domain of HDAC4 with K_d of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .

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 .

HY-N10578

Genkwadaphnin	Others	Cancer
Genkwadaphnin is a daphnane diterpenoid, targeting of importin-β1 to reduce the nuclear accumulation of key CRPC drivers, and shut down their downstream oncogenic signaling. Genkwadaphnin shows potent anti-tumor activity and inhibits castration-resistant prostate cancer (CRPC) in vivo in mice .

HY-109050

Alobresib 1 Publications Verification GS-5829	Epigenetic Reader Domain	Cancer
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .

HY-P99802

Pasotuxizumab BAY 2010112; AMG 212	CD3	Cancer
Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with K_Ds 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) .

HY-139970

VPC-13789	Androgen Receptor	Endocrinology Cancer
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) .

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) .

HY-124573

OBI-3424 TH-3424	DNA Alkylator/Crosslinker	Cancer
OBI-3424 (TH-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research .

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) .

HY-119001

BKM1644	Others	Cancer
BKM1644, an acyl-tyrosine bisphosphonate amide derivative, exhibits potent anti-cancer activity. BKM1644 effectively inhibits the proliferation of metastatic, castration-resistant prostate cance (mCRPC) cells. BKM1644 sensitizes mCRPC cells to Docetaxel (HY-B0011) and retards the bone metastatic growth of prostate cance .

HY-163340

GA32	Glucocorticoid Receptor Androgen Receptor	Cancer
GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC₅₀ values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .

HY-10617

Rucaparib phosphate Maximum Cited Publications 32 Publications Verification AG-014699 phosphate; PF-01367338 phosphate	PARP	Cancer
Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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 .

HY-10617A

Rucaparib Maximum Cited Publications 32 Publications Verification AG014699; PF-01367338	PARP	Cancer
Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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 .

HY-145388

AU-15330 3 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
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 .

HY-10617D

Rucaparib acetate AG014699 acetate; PF-01367338 acetate	PARP	Cancer
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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 .

HY-10617B

Rucaparib hydrochloride AG014699 hydrochloride; PF-01367338 hydrochloride	PARP	Cancer
Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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 .

HY-102003

Rucaparib monocamsylate 2 Publications Verification AG014699 monocamsylate; PF-01367338 monocamsylate	PARP	Cancer
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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 .

HY-102003A

Rucaparib camsylate AG014699 camsylate; PF-01367338 camsylate	PARP	Cancer
Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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 .

HY-10617C

Rucaparib tartrate AG-014699 tartrate; PF-01367338 tartrate	PARP	Cancer
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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 .

HY-10528S

Tasquinimod-d3 ABR-215050-d₃	HDAC Isotope-Labeled Compounds	Cancer
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn ²⁺ binding domain of HDAC4 with K_d of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .

HY-100348

EPI-001
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .

HY-149894

MC-1-F2	Biochemical Assay Reagents	Cancer
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 .

HY-107534

AG-045572	GnRH Receptor	Endocrinology
AG-045572 is a GnRH receptor antagonist with K_is of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone .

HY-144636

Atg4B-IN-2	Atg4 Cathepsin Phospholipase Autophagy	Cancer
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with K_i 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 .

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 .

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 .

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure