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

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

RD162 is a non-steroidal antiandrogen (NSAA) specifically binding to the androgen receptor (AR).

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

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

VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX. VPC-70063 exhibits Myc-Max transcriptional activity inhibition of 106% with an IC50 of 8.9 μM and Myc-Max/UBE2C downstream pathway inhibition of 94%. VPC-70063 can be used for studies about anticancer.

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 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.

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).

CLP-3094 (2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE) is a potent androgen receptor BF3 (binding function 3) inhibitor. BF3-IN-1 inhibits AR transcriptional activity with IC50 of 4 μM. CLP-3094 is a selective and potent GPR142 antagonist.

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

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.

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.

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.

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.

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.

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 progesterone-receptor (IC50=0.2 nM) and glucocorticoid-receptor antagonist (IC50=2.6 nM). Mifepristone is used to terminate pregnancy, treat uterine fibroids, and treat endometriosis.

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

Methyl decanoate (capric acid methyl ester) is an ester compound commonly used as an intermediate in organic synthesis and widely applied in biochemical experiments.

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.

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

Monascuspiloin (Monascinol), a compound extracted from rice fermented with Rhodobacter sphaeroides, exhibits antiandrogenic and antitumor activity and inhibits the proliferation of PC-3 and LNCaP.Monascuspiloin improves lipid metabolism and hepatic function in over-alcohol-addicted mice by decreasing hepatic MDA levels and increasing hepatic CAT, SOD and GSH levels.Monascuspiloin has been shown to improve lipid metabolism and hepatic function in over-alcoholized mice. Monascuspiloin regulates the transcription and protein expression of genes related to hepatic lipid metabolism and oxidative stress, and can be used to study alcohol-induced liver injury.