androgen-induced

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.

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.

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......

MI136 是 menin-MLL(PPI) 蛋白互作的抑制剂，其 IC50值为31 nM，Kd 值为23.6 nM。它可抑制 DHT 诱导的雄激素受体 (AR) 靶基因的表达，有用于去势抵抗性肿瘤的潜能。

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)

Androgen receptor antagonist 4 (Compound AT2) 表现出抗癌活性。Androgen receptor antagonist 4 有效拮抗 AR 的转录活性，抑制 AR 的下游靶基因，并阻断 DHT 诱导的 AR 核转位。它是雄激素受体 (AR) 的拮抗剂 (IC50 = 0.15 μM)。

Cyproterone acetate (Cyproterone 17-O-acetate) 是能够抗雄激素(IC50=7.1 nM) 和孕激素合成的类固醇。它与 progesteron 和糖皮质激素受体有亲和力。

MDG506是一种新型的选择性AR相互作用干扰剂，其在PCa模型中显示出低细胞毒性，并呈现出剂量响应性地降低经典抗雄激素诱导的前列腺特异性抗原表达。

ABC34 is an inactive control probe for JJH260 , the inhibitor of androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). ABC34 demonstrates an IC50 value greater than 25 μM for the inhibition of 9-PAHSA but is more potent in blocking the serine hydrolase ABHD6 and the palmitoyl-protein hydrolase PPT1, which are both off-targets of JJH260.

JNJ-pan-AR, a meylated analogue of JNJ-63576253, is a novel pan-AR antagonist with potent activity against wild-type and clinically relevant AR mutations including F877L. JNJ63576253, also known as TRC253, is a potent and orally active androgen receptor antagonist. TRC253 specifically binds to both wild-type and certain mutant forms of AR, thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus.

Gartanin 是山竹果中的一种天然黄酮，具有抗氧化、抗真菌、抗炎、神经保护和抗肿瘤活性。它能够诱导人脑胶质瘤细胞的细胞周期阻滞和自噬，抑制其迁移。