| Bioactivity | EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer[1][2][3]. | ||||||||||||
| Invitro | EPI-001 (5-100 μM; 7 d) inhibits PCa/CRPC cell growth in a dose-dependent manner[2].EPI-001 (50 μM) inhibits endogenous AR mRNA and protein expression in PCa and CRPC cell lines[2].EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5[2]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| Name | EPI-001 | ||||||||||||
| CAS | 227947-06-0 | ||||||||||||
| Formula | C21H27ClO5 | ||||||||||||
| Molar Mass | 394.89 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|