lncap

Enzalutamide (MDV3100) 是一种雄激素受体 (AR) 拮抗剂 (IC50=36 nM in LNCaP)。Enzalutamide 可以激活自噬，具有抗肿瘤活性，常用于去势抵抗性前列腺癌的治疗。

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

ONC1-13B 是一种高效的雄激素受体（AR）拮抗剂，对雄激素敏感的人 PCa LNCaP 细胞中抑制 PSA 产生的ic50在 59-80 nM范围内。

ABBV-744 是一种 BDII 选择性 BET 溴结构域抑制剂，可抑制 BRD2 3 4。 它可研究炎症性疾病、癌症和艾滋病。

Amygdalin (Laetrile) 是一种植物葡萄糖苷，分离自蔷薇果实的果核中，如杏，桃，杏仁，樱桃和李子。

Abacavir (Ziagen) 是一种核苷类似物逆转录酶抑制剂。

Abacavir sulfate (Ziagen) 是一种核苷类似物逆转录酶抑制剂，可用于 HIV 和 AIDS。

JNJ-63576253 free base (TRC253) 是具有口服活性的、有效的雄激素受体的完全拮抗剂，在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的 IC50值分别为 37 和 54 nM。它可用于研究去势抵抗性前列腺癌 (CRPC) 。

VPC-13163 (NSC-52361) 对 LNCaP 和耐恩杂鲁胺的前列腺癌细胞系 (MR49F) 具有很强的抗增殖活性，而它不影响 AR 独立 PC3 细胞系的生长。它还抑制 LNCaP 和 MR49F 中的前列腺特异性抗原 (PSA) 并降低 AR 靶基因 PSA 和 TMPRSS2 的表达。这些发现表明 VPC-13566 表现出 AR BF3 特定的作用机制。

mTOR inhibitor 9d 是一种蛋白激酶 mTOR 和PI3K 双重抑制剂，对mTOR 的IC50值为0.31nm，可用于治疗白血病、皮肤癌、乳腺癌、肺癌和结肠癌。

VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) 是 c-Myc-MAX 的抑制剂。 VPC-70063 的 Myc-Max 转录活性抑制率为 106%，IC50 为 8.9 μM，Myc-Max/UBE2C 下游通路抑制率为 94%。 VPC-70063 可用于抗癌研究。

mTOR inhibitor 9a 对人LNCap 细胞的生长具有抑制作用，ic50为80nm。mTOR inhibitor 9a 可能具有抗肿瘤活性。

AR antagonist 1 是 AR 拮抗剂，能够与 E3 连接酶配体结合，与 VHL 蛋白结合亲和力较弱，用于 PROTACARD-266 合成。

Bexlosteride (LY300502) 是一种苯并喹啉酮类人 I 型 5α-还原酶抑制剂。Bexlosteride 在 LNCaP 细胞培养物中显示出代谢抑制、抗增殖和抗分泌作用。Bexlosteride 可用于前列腺癌的研究。

NSC348884 是一种核磷蛋白抑制剂，可破坏寡聚体形成并诱导细胞凋亡，在不同的癌细胞系中以 IC50 为 1.7-4.0 μM 抑制细胞增殖。

HPOB 是一种高选择性HDAC6抑制剂，IC50为 56 nM，其选择性是其他 HDAC 的 30 倍以上。它提高 DNA 损伤抗癌药物在转化细胞中的有效性。

CLP-3094 (2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE) 是一种雄激素受体 BF3(binding function 3) 抑制剂，是一种选择性GPR142拮抗剂。BF3-IN-1 抑制 AR 转录活性 (IC50:4 μM)。

SK33 是一种有效的组织选择性抗雄激素药物，是一种肌醇类似物，能够降低雄激素受体 (AR) 的转录活性。

RD162 是一种与雄激素受体 (AR) 特异性结合的非甾体抗雄激素 (NSAA)。

12-O-Methylcarnosic acid 是分离自小叶丹参的丙酮提取物的一种二萜肉桂酸，可抑制 5α-还原酶 (5α-reductase) 活性，IC50为 61.7 μM。它抑制 LNCaP 细胞的增殖。它具有抗微生物活性、抗氧化和抗癌活性。

IPI-9119 是一种具有口服活性、选择性和不可逆的 FASN 抑制剂 (IC50 = 0.3 nM)。

9-Methoxycanthin-6-one 是存在于完整植株和不同外植体的愈伤组织中的 Canthin-6-one 生物碱，具有抗肿瘤作用。

HDAC-IN-64 (Compound 13) 为HDAC抑制剂，对HDAC4/6的IC50值为24 nM及85 nM。其对前列腺癌（PCA）细胞表现出抗增殖与抗迁移效果，并能抑制LNCaP和RWPE-1细胞的生长，GI50值分别达到0.32 μM与1.1 μM。

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].

JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC50 value of 0.57 μM. JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 μM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2. JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.

Y08060 is an effective and selective BET Inhibitor for the Treatment of Prostate Cancer. Y08060 effectively suppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC in prostate cancer cell lines. Y08060 has IC50 values of 3.23 and 4.41 μM in inhibition of cell viability in the C4 2B and LNCaP cell lines, respectively.

Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells (IC50s = 1.1, 72.5, 77, and 24.5 nM, respectively).

Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50 = 13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC50 = 1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC50s = 34.3, 47, and 37.2 μg ml, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50 = 0.84 μg ml) and increases survival of P. densiflora trees inoculated with B. xylophilus.

Dual cyclooxygenase-2 (COX-2) 5-lipoxygenase (5-LO) inhibitors are potential therapeutic agents for inflammatory diseases and for prostate cancer. CAY10416 is a dual COX-2 5-LO inhibitor with IC50 values of 50 and 3 nM, respectively. The selectivity of CAY10416 for COX is greater than 200-fold for COX-2 versus COX-1. COX-2 5-LO inhibitors such as CAY10416 are also apoptosis-inducing agents and are potentially useful in prostate cancer chemotherapy. In the PC3 human carcinoma cell line, CAY10416 exhibits a 45% inhibition of proliferation at 100 μM. In the LNCaP human carcinoma cell line, CAY10416 inhibits growth with an IC50 value of 83 μM.

Enzalutamide D3 is a deuterium labeled Enzalutamide . Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

Dihydrodaidzin shows cytotoxic activities against human stomach carcinoma (Hs 740.T, Hs 756 T), breast adenocarcinoma (Hs 578 T, Hs 742.T), and prostate carcinoma (DU 145, LNCaP-FGC) cell lines.

ARD-69 is a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent mann

Antitumor agent-120 (compound 1) 为一类黄酮化合物，来源于葛根提取。本化合物对LNCaP和PC3癌细胞的抑制作用不明显，表现出IC50s均大于50 μM。

AR AR-V7-IN-1 (Compound 20i) 作为一种有效的AR AR-V7抑制剂，其 IC50 值为 172.85 nM。在 LNCaP 和 22RV1 细胞系中，该化合物的 IC50 值分别为 4.87 μM 和 2.07 μM，有效抑制了细胞生长。此外，AR AR-V7-IN-1 在 22RV1 异种移植模型中显著抑制肿瘤生长，表明其在前列腺癌研究中的潜在应用价值。

MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2/M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0/G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V/PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......

LSD1-IN-16 (compound 4b) 是 LSD1的有效抑制剂，可抑制 LSD1-CoREST、MAO-A 和 MAO-B，IC50值分别为 0.015、0.024 和 0.366 μM。LSD1-IN-16 在前列腺癌 LNCaP 细胞中表现出细胞生长阻滞，IC50值为 15.2 μM。

XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kinase activation and anchorage-independent growth in NIH 3T3 transformed with v12 H-ras. Since the antiproliferative effect of the compound is not related to the ras phenotype, XR3054 may also have effects on other cell signaling mechanisms.

BET-IN-16 (Comp I) 是一种BET抑制剂，展现出抗癌活性。BET-IN-16抑制前列腺癌细胞的生长，其对LNCaP和22Rv1细胞的IC50值分别为0.043 μM和0.034 μM。

Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatocellular carcinoma cells when used at a concentration of 4 μM.3 1.Qian-Cutrone, J., Huang, S., Shu, Y.-Z., et al.Stephacidin A and B: Two structurally novel, selective inhibitors of the testosterone-dependent prostate LNCaP cellsJ. Am. Chem. Soc.124(49)14556-14557(2002) 2.Wulff, J.E., Herzon, S.B., Siegrist, R., et al.Evidence for the rapid conversion of stephacidin B into the electrophilic monomer avrainvillamide in cell cultureJ. Am. Chem. Soc.129(16)4898-4899(2007) 3.Hu, L., Zhang, T., Liu, D., et al.Notoamide-type alkaloid induced apoptosis and autophagy via a P38/JNK signaling pathway in hepatocellular carcinoma cellsRSC Adv.9(34)19855-19868(2019)

1,4-O-Diferuloylsecoisolariciresinol(9,9'-Di-O-(E)-feruloylsecoisolariciresinol),and pierreione B, two novel inhibitors of mTOR signaling, have strong anticancer activity. (+)-9,9'-O-Diferuloylsecoisolariciresinol has significant cytotoxic activity agains

ARD-266 is a highly potent VHL E3 ligase-based androgen receptor (AR) PROTAC degrader, effectively inducing AR protein degradation in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines (DC50s: 0.2-1 nM).

Neochamaejasmin A can inhibit cellular (3)H-thymidine incorporation (IC 50 12.5 microg mL) and subsequent proliferation of human prostate cancer LNCaP cells, it blocks cell cycle progression at the G1 phase by activating the p21 protein and ultimately pro

Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2 M phase. Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation. [2] Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg kg every other day.[1]

BWA-522是一种口服有效的小分子PROTACs，针对AR-FL和AR-V7显示出显著的降解活性。该化合物通过对Androgen Receptor的AR-NTD进行拮抗，诱发PC细胞的apoptosis。在LNCaP异种移植模型中，BWA-522以每日60 mg/kg的剂量口服给药，实现了76%的肿瘤生长抑制(TGI=76%)。在VCaP和LNCaP细胞系中对AR-V7和AR-FL的降解效率分别达到77.3%(1 μM)和72.0%(5 μM)。

MC2652 (compound 1a) 是 LSD1的有效抑制剂，在白血病细胞 MV4-11 和 NB4 中表现出高抑制作用。MC2652 对前列腺癌的 LNCaP 细胞表现出抗增殖活性。

(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MICs = 0.16-0.21 μg/ml). It inhibits polymerization and the GTPase activity of E. coli FtsZ, a tubulin-like GTPase involved in bacterial cell division (IC50s = 8.2 and 7 μg/ml, respectively). (-)-Viriditoxin inhibits proliferation of human DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5.36, 0.63, and 7.6 μM, respectively) . It is also toxic to mice (LD50 = 2.8 mg/kg, i.p.).

Fadolmidine, also known as MPV-2426, is a novel and potent alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia. Fadolmidine displayed high affinity and full agonist efficacy at all three human alpha2-adrenoceptor subtypes (A, B and C) in transfected CHO cells with EC50 values (nM) of 0.4, 4.9 and 0.5, respectively. Fadolmidine inhibited also electrically evoked contractions in rat vas deferens demonstrating the activation of rodent presynaptic alpha2D-adrenoceptors with an EC50 value of 6.4 nM. Moreover, fadolmidine was a full agonist at human alpha1A-adrenoreceptor (EC50 value 22 nM) and alpha1B-adrenoreceptor (EC50 value 3.4 nM) in human LNCaP cells and transfected HEK cells, respectively. Agonism at the alpha1-adrenoceptor was also observed in rat vas deferens preparations although at lower potency (EC50 value 5.6 microM). Fadolmidine demonstrated potent alpha2-adrenoceptor agonist activity also in vivo by inhibiting electrically induced tachycardia i......

Androgen receptor antagonist 5 是雄激素受体 (AR) 的有效拮抗剂 (IC50: 6.17 μM)。Androgen receptor antagonist 5 能够有效损害 AR 核转位，减少细胞核 AR 水平，扰乱 AR 介导的基因调控。Androgen receptor antagonist 5 对前列腺癌细胞 LNCaP 的增殖具有抑制作用，并在 LNCaP 异种移植小鼠模型中显示出抗肿瘤效果，能够用于研究前列腺癌症。