prostate tumor

Sabizabulin (ABI-231) is a potent, orally bioavailable α- and β-tubulin inhibitor that is active against melanoma and prostate cancer cell lines. Sabizabulin inhibits tumor growth and metastatic phenotypes of cervical cancer cells by targeting HPV E6 and E7 and is also being studied in prostate cancer.

Isomer-Turosteride (Isomer-Turosteride(Isomer-137099-09-3)) is a novel 5 alpha-reductase inhibitor.The antiprostatic effect of Isomer-Turosteride in adult rats is associated with the inhibition of the conversion of T to DHT.Isomer-Turosteride induces a decrease in prostate DHT independent of a secondary increase in T. Isomer-Turosteride has anticancer activity and inhibits the growth of tumor cells. Turosteride has anticancer activity and inhibits the growth of tumor cells. Translated with www.DeepL.com Translator (free version)

BMS-986365 (CC-94676) is an orally available, selective and highly potent AR degrader with potential anticancer activity that inhibits AR signaling and suppresses tumor growth for the study of prostate cancer.

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) is a strong trypsin inhibitor and a relatively weak inhibitor of urokinase type plasminogen activator (uPA) (K i =82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice [1] [2].

Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

OB 24 hydrochloride is a potent and selective heme oxygenase 1 (HO-1) inhibitor (IC50 values are 1.9 and >100 μM for HO-1 and HO-2 respectively), reduces protein carbonylation and reactive oxygen species formation in advanced prostate cancer cells (PCA). Inhibits cell proliferationin vitroand PCA tumor growth and lymph node/lung metastasesin vivo. Synergizes with Taxol.

Tanespimycin (KOS 953) (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM).

GDC-2992 is a selective and oral AR (androgen receptor) degrader that inhibits the proliferation of tumor cells overexpressing AR, degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, and can be used for oncology studies in denuded resistant prostate cancer (CRPC).

Chemically modified tetracyclines (CMTs) can inhibit MMPs, but lack antimicrobial activity. Nonantimicrobial derivative of tetracycline called incyclinide (COL-3, CMT-3). Incyclinide (CMT-3) has been shown to experimentally suppress prostate cancer, colon adenocarcinoma and melanoma invasiveness in cell culture and to inhibit tumor growth and metastasis.

MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.

Lu-AAZTA-NI-PSMA-093, a bivalent radiopharmaceutical agent designed for prostate cancer treatment, improves tumor targeting and retention. This is achieved by integrating a hypoxia-sensitive nitroimidazole (NI) group with a prostate-specific membrane antigen (PSMA) targeting moiety.

FL442 is an Androgen Receptor (AR) modulator. This compound exhibits potent inhibitory effects in AR-dependent prostate cancer cells, showing similar suppression efficiency to the traditional antiandrogen drugs Bicalutamide and Enzalutamide. It also maintains antiandrogen activity against the Enzalutamide-resistant AR mutant F876L. The pharmacokinetic properties of FL442 in mice reveal a longer half-life (8 hours), excellent targeting (prostate tissue), and metabolic stability. Additionally, it is effective at inhibiting LNCaP tumor growth at low plasma concentrations (30 ng mL).

LX1, an anti-prostate cancer compound, specifically targets the androgen receptor (AR), AR variants, and the steroidogenic enzyme AKR1C3. It inhibits AKR1C3's enzymatic function, decreases the conversion of androstenedione to testosterone, and reduces the expression of both AR and AR-V7, subsequently downregulating their target genes. Additionally, LX1 is effective in overcoming tumor cell resistance to Enzalutamide, and when combined with Enzalutamide, it further suppresses tumor growth.

ML234 is a dual inhibitor targeting EZH2 LSD1, with IC50 values of 0.09 and 0.12 μM, respectively. It demonstrates strong antiproliferative effects on prostate cancer cell lines LNCAP, PC3, and 22RV1. Additionally, ML234 inhibits tumor growth in a 22RV1 xenograft mouse model, showing potential as a research agent in prostate cancer therapeutics.

YJ9069 is a selective CDK12 CDK13P ROTAC degrader with an IC50 of 22.22 nM in VCaP cells. Rapid degradation of CDK12 13 by this compound triggers transcription elongation defects dependent on gene length, leading to DNA damage and cell cycle arrest. YJ9069 effectively inhibits the proliferation of prostate cancer cell subpopulations and significantly suppresses prostate tumor growth in vivo.

Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.

Compound EF2 (Androgen receptor antagonist 12) is an orally active antagonist of the androgen receptor (AR) with an IC50 of 0.30 µM. It inhibits the transcriptional activity of mutant AR and the proliferation of AR-positive PCa (prostate cancer) cell lines. Additionally, Compound EF2 blocks the nuclear translocation of AR and suppresses tumor growth in the C4-2B xenograft mouse model. This compound is used for research in prostate cancer.

AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.

DTS-201 sodium (CPI-0004Na) is a peptide prodrug of Doxorubicin. It contains a tetrapeptide segment that is hydrolyzed by endopeptidases in the tumor microenvironment to produce metabolites, which are then converted into active Doxorubicin upon cellular entry. DTS-201 has demonstrated antitumor efficacy in xenograft models of prostate, breast, and lung cancers.

LYG-409 is an orally active GSPT1 degrader. It demonstrates exceptional in vivo anti-tumor activity against acute myeloid leukemia and prostate cancer, with tumor growth inhibition rates (TGI) of 94.34% and 104.49%, respectively. LYG-409 inhibits KG-1 cells by degrading GSPT1, with an IC50 of 9.50 nM and a DC50 of 7.87 nM in vitro.

Estramustine (LEO-275) is a nitrogen mustard linked to estradiol, usually as phosphate. Estramustine has been used to treat prostatic neoplasms; also has radiation protective properties. Estramustine is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.

XY018 is an orally available, selective and highly effective ROR-γ antagonist with antitumor activity, inhibits ROR-γ activity, inhibits tumor cell growth, and can be used to study drug-resistant prostate cancer.