|DY131,also known as GSK-9089,is a novel selective agonist at estrogen-related receptors ERRβ and ERRγ.DY131 could potentiate the ERRgamma-induced growth inhibition in LNCaP-ERRgamma and DU145-ERRgamma cells in a dose-dependent manner.ERRgamma may perform an antiproliferative or tumor-suppressing function in prostate cancer cells.
|Endoxifen is a secondary metabolite of tamoxifen.It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.
|Ostarine(GTx-024,MK-2866)is a selective androgen receptor modulator (SARM)with Ki of 3.8 nM,and is tissue-selective for anabolic organs.
|Walrycin B CAS:878419-78-4
|Walrycin B is a potent WalR inhibitor.The WalK/WalR(YycG/YycF)two-component system,which is essential for cell viability,is highly conserved and specific to low-GC percentage of Gram-positive bacteria,making it an attractive target for novel antimicrobial compounds.
|AZD1981is an orally available selective CRTH or DP2 antagonist currently in clinical development for asthma.AZD1981 blocks functional responses in eosinophils,Th2 cells and basophils.AZD1981 displaced radio-labelled PGD2 from human recombinant DP2 with high potency(pIC50=8.4).Binding was reversible,non-competitive and highly selective against a panel of more than 340 other enzymes and receptors,including DP1(>1000-fold selective).AZD1981 inhibited DP2-mediated shape change and CD11b up-regulation in human eosinophils,shape change in basophils and chemotaxis of human eosinophils and Th2 cells with similar potency.AZD1981 exhibited good cross-species binding activity against mouse,rat,guinea pig,rabbit and dog DP2.Evaluation in mouse,rat or rabbit cell systems was not possible as they did not respond to DP2 agonists.Agonist responses were seen in guinea pig and dog, and AZD1981 blocked DP2-mediated eosinophil shape change.Such responses were more robust in the guinea pig,where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow.
|Andarine(GTx-007,S-4)is a selective non-steroidal androgen receptor(AR)agonist with Ki of 4 nM,tissue-selective for anabolic organs.
|Testolone (RAD140) CAS：1182367-47-0
|Testolone(RAD140)is a potent,orally bioavailable,nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.
|ODM-201,also known as Darolutamide,ODM-201 is a full and high-affinity AR antagonist that,similar to second-generation antiandrogens enzalutamide and ARN-509,inhibits testosterone-induced nuclear translocation of AR.Importantly,ODM-201 also blocks the activity of the tested mutant ARs arising in response to antiandrogen therapies.
|RU-58841 is a new specific topical antiandrogen:a candidate of choice for the treatment of acne,androgenetic alopecia and hirsutism.The potent localized inhibition of sebaceous glands by RU 58841 demonstrates the excellent potential of this compound as a topical drug for the treatment of acne and other androgen-mediated disorders.
|Dimethylcurcumin(ASC-J9,Dimethyl curcumin,GO-Y025)is an androgen receptor (AR)degradation enhancer that suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.