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Results for "

castration-resistant prostate cancer (CRPC)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) 17β-HSD (1) Androgen Receptor (15) Apoptosis (8) Biochemical Assay Reagents (1) c-Met/HGFR (1) Cytochrome P450 (2) Drug Metabolite (1) Endothelin Receptor (2) Epigenetic Reader Domain (3) Estrogen Receptor/ERR (1) Fatty Acid Synthase (FASN) (1) Histone Methyltransferase (1) Isotope-Labeled Compounds (2) Ligands for E3 Ligase (3) MNK (1) Molecular Glues (2) PARP (10) Prostaglandin Receptor (1) PROTACs (2) Reference Standards (4) ROR (1)
By Research Areas:	Cancer (43) Endocrinology (3)

By Targets:

11β-HSD (1)

17β-HSD (1)

Androgen Receptor (15)

Apoptosis (8)

Biochemical Assay Reagents (1)

c-Met/HGFR (1)

Cytochrome P450 (2)

Drug Metabolite (1)

Endothelin Receptor (2)

Epigenetic Reader Domain (3)

Estrogen Receptor/ERR (1)

Fatty Acid Synthase (FASN) (1)

Histone Methyltransferase (1)

Isotope-Labeled Compounds (2)

Ligands for E3 Ligase (3)

MNK (1)

Molecular Glues (2)

PARP (10)

Prostaglandin Receptor (1)

PROTACs (2)

Reference Standards (4)

ROR (1)

By Research Areas:

Cancer (43)

Endocrinology (3)

Inhibitors & Agonists

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: PSMA BCRP

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

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-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) .

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 .

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-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-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-145388

AU-15330 5+ Cited Publications	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-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-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-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-70006

Galeterone 3 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-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-10088R

Zibotentan (Standard) ZD4054 (Standard)	Reference Standards Endothelin Receptor Apoptosis	Endocrinology Cancer
Zibotentan (Standard) is the analytical standard of Zibotentan. This product is intended for research and analytical applications. 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 .

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-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-111061

GTX-758	Estrogen Receptor/ERR	Cancer
GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research .

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-10617

Rucaparib phosphate 40+ Cited Publications 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 44 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-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-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-161700

BMS-737	Cytochrome P450	Cancer
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 .

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-102003

Rucaparib monocamsylate 35+ Cited Publications 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-174908

SJL2-1	Histone Methyltransferase 11β-HSD Androgen Receptor	Cancer
SJL2-1 is a PRMT5 inhibitor, with an IC₅₀of 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) .

HY-10617AR

Rucaparib (Standard) AG014699 (Standard); PF-01367338 (Standard)	Reference Standards PARP	Cancer
Rucaparib (Standard) is the analytical standard of Rucaparib. This product is intended for research and analytical applications. 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 .

HY-10617R

Rucaparib phosphate (Standard) AG-014699 phosphate (Standard); PF-01367338 phosphate (Standard)	Reference Standards PARP	Cancer
Rucaparib (phosphate) (Standard) is the analytical standard of Rucaparib (phosphate). This product is intended for research and analytical applications. 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 .

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-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 .

HY-10617AS

Rucaparib-d8 AG014699-d₈ ; PF-01367338-d₈	Isotope-Labeled Compounds PARP	Cancer
Rucaparib-d₈ (AG014699-d₈ ) is deuterium labeled Rucaparib. 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-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-N0790

Lupeol 4 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-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-W744741

Lupeol-d3	Isotope-Labeled Compounds Androgen Receptor Apoptosis	Cancer
Lupeol-d₃ is the deuterium labeled Lupeol (HY-N0790). Lupeol 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-N0790R

Lupeol (Standard) Clerodol (Standard); Monogynol B (Standard); Fagarasterol (Standard)	Reference Standards Androgen Receptor Apoptosis	Cancer
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. 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-403733B

(+)-JJ-450	Androgen Receptor Prostaglandin Receptor	Cancer
(+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003) .

HY-403733A

(–)-JJ-450	Androgen Receptor	Cancer
(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR ^F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .

HY-163410

AU-24118 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .

HY-403733C

JJ-450	Androgen Receptor	Cancer
JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR ^F876L. JJ-450 has an IC₅₀ of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR ^F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .

HY-170820

XYD049	Molecular Glues	Cancer
XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC₅₀=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC₅₀=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .

HY-155666

YXG-158	Androgen Receptor	Cancer
YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC₅₀ value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC₅₀ value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer .

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 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. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .

Cat. No.	Product Name	Target	Research Area