crpc

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

IPI-9119 is an orally active, selective, and irreversible FASN inhibitor (IC50 = 0.3 nM).

AKR1C3-IN-4, a potent and selective inhibitor of aldo-keto reductase 1C3 (AKR1C3) with an IC50 of 0.56 μM, shows potential for castrate-resistant prostate cancer (CRPC) research.

Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.

JNJ-63576253 free base (TRC253) 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 is a Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

KB-0742 dihydrochloride is a potent, selective, and orally administered inhibitor of CDK9.

Proxalutamide is a potent antagonist of the androgen receptor (AR).

Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD), inhibiting AR transcriptional activity with an IC50 value of 7.4 μM. Ralaniten exhibits anticancer activity and is used to study desmoplasia-resistant prostate cancer (CRPC).

MC-1-F2 is a direct FOXC2 inhibitor with anticancer activity, inhibits cancer stem cell (CSC) characteristics, and reduces the invasive ability of castration-resistant prostate cancer (CRPC) cell lines. MC-1-F2 can be used to study prostate cancer.

Rucaparib (PF-01367338) is a PARP protein inhibitor (PARP-1 Ki=1.4 nM) and hexose hexose-6-phosphate dehydrogenase (H6PD) inhibitor with oral activity. Rucaparib exhibits antitumor activity, with activity against desmoplasia-resistant prostate cancer (CRPC).

GDC-2992 is a selective and orally active androgen receptor (AR) degradator that degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, making it suitable for studying castration-resistant prostate cancer (CRPC).

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.

Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.

Compound Z15 (ZNU-IMB-Z15) acts as an antagonist and degrader of the androgen receptor (AR). It inhibits the proliferation of castration-resistant prostate cancer (CRPC) cell lines that are AR-positive and induces apoptosis. Compound Z15 exhibits anticancer activity both in vivo and in vitro.

(+)-JJ-74-138 is a novel non-competitive androgen receptor (AR) antagonist capable of inhibiting enzalutamide-resistant castration-resistant prostate cancer (CRPC).

VPC-80051 is an hnRNP A1 splicing activity inhibitor that directly interacts with the hnRNP A1 RBD and reduces AR-V7 messenger levels in the 22Rv1 CRPC cell line. VPC-80051 is applicable in prostate cancer research.

XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1, with a DC50 of 19 nM, used for researching MYC-driven castration-resistant prostate cancer (CRPC). It effectively inhibits the growth of 22Rv1 cells (IC50 = 7 nM) and exhibits antitumor efficacy in vivo. XYD049 downregulates CRPC-associated oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 comprises a molecular glue linker (black part) NH2-C5-NH-Boc, a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a target protein ligand (red part) GSPT1 ligand-1, with the E3 ligase ligand + linker forming the conjugate E3 Ligase Ligand-linker Conjugate 158.

SPA-10091-HCl is a DOT1L degrader that selectively degrades the DOT1L protein via the nuclear ubiquitin-proteasome pathway, thereby inhibiting H3K79 methylation in CRPC cells. It also inhibits DOT1L enzymatic activity (IC50 = 0.87 μM), induces apoptosis, and significantly suppresses tumor growth in vivo.

HDAC6-IN-32 (compound 25202) is a selective and potent inhibitor of HDAC6. It blocks HDAC6 activity and disrupts microtubule dynamics, which leads to spindle assembly checkpoint (SAC) activation and prolonged mitotic arrest, ultimately causing apoptosis in CRPC cells.

(+)-JJ-450 is a non-competitive antagonist that targets the androgen receptor (AR), inhibiting nuclear localization and transcriptional activity of AR under androgen-deprived conditions. In LN95 cells, (+)-JJ-450 is less effective than (-)-JJ-450 at inhibiting prostate-specific antigen (PSA) expression, likely due to its targeting of the AR ligand-binding domain (LBD). The compound works by promoting degradation of unbound AR within the nucleus and reducing AR binding to androgen response elements (AREs), thus inhibiting the transcriptional activity of AR and its splicing variants like ARv7. Additionally, (+)-JJ-450 is applicable for research in castration-resistant prostate cancer (CRPC) that is resistant to Enzalutamide (MDV3100).

JJ-450 is a non-competitive antagonist that targets androgen receptors (AR), capable of inhibiting the transcriptional activity of both wild-type AR and mutant ARF876L. It demonstrates an IC50 of approximately 1-10 μM for suppressing AR transcriptional activity in PC3 cells and selectively binds to AR without competing for the ligand binding domain (LBD) with androgens. JJ-450 functions by inhibiting the nuclear translocation of AR and promoting the degradation of unbound ligand AR within the nucleus, thereby suppressing the transcriptional activity of AR and its splice variants, such as ARF876L. This compound can be utilized in studies of castration-resistant prostate cancer (CRPC) that are resistant to Enzalutamide (MDV3100).

SJL2-1 is a PRMT5 inhibitor with an IC50 value of 1.56 μM. It suppresses the proliferation, migration, and invasion of prostate cancer cells and induces apoptosis while causing cell cycle arrest at the G0/G1 phase. SJL2-1 targets intracellular PRMT5, inhibiting androgen receptor methylation and expression. It is applicable in research on early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC).