SX-682 is a potent, selective and orally bioavailable inhibitor of CXCR1/2 ,has the potential to treat castration-resistant prostate cancer.

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).

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

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

Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.

Genkwadaphnin, a daphnane diterpenoid, targets importin-β1, reducing the nuclear accumulation of CRPC drivers and suppressing downstream oncogenic signaling. Demonstrating potent anti-tumor effects, it inhibits castration-resistant prostate cancer (CRPC) in vivo in mice [1].

Emibetuzumab is a potent humanized bivalent MET antibody (IgG4 type). Emibetuzumab has antitumor activity, inhibition of HGF-dependent and independent MET pathway activation and tumor growth, and can be used to study advanced castration-resistant prostate cancer.

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

Rilotumumab (AMG 102) is a monoclonal antibody targeting hepatocyte growth factor that inhibits HGF/ MET-driven signaling. Rilotumumab has antitumor effects and can be used to study castration-resistant prostate cancer (CRPC) and gastric cancer.

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is a chemical compound utilized in the synthesis of ARV-771, an exceptionally potent BET protein degrader. This compound selectively degrades BET protein in cells resistant to castration, exhibiting a remarkable DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, (S,R,S)-AHPC-Me hydrochloride serves as the VHL ligand derived from (S,R,S)-AHPC for the recruitment of von Hippel-Lindau (VHL) protein.

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

Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.

Dimethylcurcumin (ASC-J9) (ASC-J9) is an androgen receptor degradation enhancer. It effectively suppresses castration-resistant prostate cancer cell proliferation and invasion.

HG122 is a chemical compound that effectively facilitates the degradation of androgen receptor (AR) via the proteasome pathway, leading to the inhibition of castration-resistant prostate cancer.

VPC-13789 is a highly potent, selective, and orally bioavailable antiandrogen compound that shows promise for studying and developing therapeutics for castration-resistant prostate cancer (CRPC). In LNCaP cells, VPC-13789 effectively inhibits the transcriptional activity of the androgen receptor (AR) with an IC50 value of 0.19 μM [1].

Rucaparib (AG014699) acetate is a highly effective oral inhibitor of PARP proteins, specifically targeting PARP-1, PARP-2, and PARP-3, with a Ki value of 1.4 nM for PARP1. Additionally, it exhibits inhibitory action on hexose-6-phosphate dehydrogenase (H6PD) to a moderate extent. Rucaparib acetate shows promise in the field of research for castration-resistant prostate cancer (CRPC). [1] [2] [3] [4]

RLA-4842, an iron activator with anti-androgen properties, exhibits anti-proliferative effects on the metastatic castration-resistant prostate cancer (mCRPC) cell line [1].

Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting (DART) antibody that blocks both PD-1 and CTLA-4, enhancing T-cell responses. It is under investigation for the treatment of metastatic castration-resistant prostate cancer (mCRPC) [1] [2] [3].

BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.

Cabazitaxel (taxoid XRP6258) is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel.

EC1167 hydrochloride serves as the linker for EC1169, a prostate-specific membrane antigen-targeting tubulysin conjugate. EC1169 hydrochloride demonstrates potential in treating recurrent metastatic, castration-resistant prostate cancer (MCRPC) [1].

Minnelide is an effective therapy against pancreatic cancer. Minnelide Inhibits Androgen Dependent, Castration Resistant Prostate Cancer Growth by Decreasing Expression of Androgen Receptor Full Length and Splice Variants. Minnelide reduced tumor volume in multiple models of pancreatic cancer. Minnelide was a more effective drug against pancreatic cancer models. It effectively reduced tumor burden and tumor related morbidity in different unique but complementary mouse models. It reduced metastatic spread and increased survival in the different models as well.

Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.

Enzalutamide carboxylic acid is an antagonist of androgen receptor (AR) .

Orteronel ((S)-Orteronel)(TAK-700) was selected as a candidate for clinical evaluation. orteronel (TAK-700) is currently in phase III clinical trials for the treatment of castration-resistant prostate cancer.

LLS30 is an allosteric inhibitor of Galectin-1 (Gal-1). LLS30 decreases Gal-1 binding affinity to its binding partners, and potentially overcomes metastatic castration-resistant prostate cancer (mCRPC).

Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].

Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR). Bavdegalutamide can be used in studies about prostate cancer. Bavdegalutamide shows oral activity and selectivity and facilitates the ubiquitination and degradation of AR.

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

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

5,6-Dihydroabiraterone, a metabolic derivative of Abiraterone, is a potent and irreversible inhibitor of CYP17A1, exhibiting antiandrogen and antitumor activities, particularly effective against castration-resistant prostate cancer (CRPC) [1] [2].

RLA-5331 is an anti-androgen compound with iron-activating properties, demonstrating anti-proliferative effects on the metastatic castration-resistant prostate cancer (mCRPC) cell line [1].

TD-802 (Compound 33c), an androgen receptor (AR) PROTAC degrader, exhibits strong microsomal stability and demonstrates potent antitumor efficacy in vivo, making it suitable for research on metastatic castration-resistant prostate cancer [1].

Pasotuxizumab (BAY 2010112) is a bispecific T-cell engager (BiTE) targeting PSMA and CD3 with dissociation constants (K D) of 47.0 nM and 9.4 nM for PSMA and CD3, respectively. It is utilized in the study of metastatic castration-resistant prostate cancer (mCRPC) [1] [2].

EC1169 is a targeted tubulysin conjugate that utilizes EC1167 as its linker. This compound shows promise in the treatment of recurrent metastatic, castration-resistant prostate cancer (MCRPC)[1].

Histone H3K27Me1 (23-34) is a peptide fragment of histone H3 that corresponds to amino acid residues 24-35 of the human histone H3.1 and H3.2 sequences. Monomethylation of histone H3 at lysine 27 is associated with actively transcribed genes and positively correlates with H3K36 trimethylation. Levels of H3K27Me1 are increased in tumor tissue isolated from patients with metastatic hormone-na ve and castration-resistant prostate cancer. Histone H3K27Me1 (23-34) has been used in epitope mapping of the lupus-derived monoclonal antibody BT164.