lncap

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.

Abacavir sulfate (Ziagen) , a nucleoside analogue, effectively utilize its antiviral activity

HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs.

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

TRIM24 BRPF1-IN-2 is a selective dual TRIM24 BRPF1 inhibitor with anticancer activity that inhibits proliferation, gene and protein expression, and colony formation of prostate cancer cells in a dose-dependent manner.

Androgen receptor antagonist 1, an orally available full androgen receptor antagonist (IC50: 59 nM), is utilized in the synthesis of PROTAC AR degraders, achieving 24% and 47% AR protein degradation in LNCaP cells at concentrations of 1 μM and 10 μM, respectively.

Venuloside A (ESK246), a monoprostane glycoside from Pittosporum venulosum, is a LAT3 inhibitor and a leucine uptake inhibitor that inhibits the transporter of leucine through LAT3, and may be used in the study of prostate cancer.

VPC-13163 (NSC-52361) has strong anti-proliferative activity against LNCaP and Enzalutamide-resistant prostate cancer cell lines (MR49F) whereas it did not affect the growth of AR independent PC3 cell line. It also inhibits Prostate Specific Antigen (PSA) in both LNCaP and MR49F and reduces expression of AR target genes, PSA and TMPRSS2. These findings suggest that VPC-13566 exhibits AR BF3 specific mechanism of action.

mTOR inhibitor 9a inhibited the growth of human LNCap cells with an ic50 of 80 nm. 1-methyl-3 -{4-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)thieno[3,2-d]pyrimidin-2-yl]phenyl}urea may have antitumor activity.

Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.

ONC1-13B is a potent androgen receptor (AR) antagonist with an ic50 in the range of 59-80 nM that inhibits PSA production in androgen-sensitive human PCa LNCaP cells.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2 3 4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Amygdalin (Laetrile) has antifibrotic, antitumor, anti-inflammatory and analgesic effects, amygdalin joint HSYA could inhibit the degeneration of the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and better than the single use of Amygdalin or HSYA. Amygdalin induces apoptotic cell death in human DU145 and LNCaP prostate cancer cells by caspase-3 activation through down-regulation of Bcl-2 and up-regulation of Bax.

4-Isopropoxybenzaldehyde (compound 16), a powerful ALDH1A3 inhibitor with an IC50 of 0.26 μM (cell free assay), serves as an effective ALDH3A1 substrate. But shows weak antiproliferative effect against PC3, LNCaP, and DU145 PCa cell lines with IC50>200 μM[1].

Docetaxel (RP-56976), a semi-synthetic analog of paclitaxel, is a microtubule depolymerization inhibitor (IC50=0.2 μM) that attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.

Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Adavosertib (MK-1775) is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint.

Vipivotide tetraxetan (PSMA-617) is a highly potent inhibitor of prostate-specific membrane antigen (PSMA) with a Ki of 0.37 nM.

EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).[1]

NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.

Calcitriol (1,25-Dihydroxyvitamin D3) is a metabolite of vitamin D and a vitamin D receptor (VDR) agonist (IC50=0.4 nM). Calcitriol increases intestinal absorption of calcium and phosphorus, and increases bone resorption with parathyroid hormone.

C75 is an inhibitor synthetic fatty-acid synthase (FASN) and inhibits prostate cancer cells PC3 (IC50: 35 μM).C75 increases CPT1 activity and reduces DIO.

SK33 is a potent and tissue selective anti-androgen agent. SK33 reduces androgen receptor (AR) transcriptional activity.