| Name | EPI-001 |
| Description | EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator. |
| Cell Research | LNCaP cells are treated with bicalutamide (BIC) or EPI-001 for 1 hr before the addition of R1881 (0.1 nM) for 4 days. LNCaP cells are treated with OCM (50%) with, or without, EPI-001 for 3 days (serum-free, androgen-free, phenol red-free conditions).(Only for Reference) |
| In vitro | EPI-001 blocks transactivation of the AR NTD, interacts with the AF-1 region, inhibits protein-protein interactions with AR, and reduces AR interaction with androgen-response elements on target genes. In LNCaP cells, EPI-001 inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. [1] In LNCaP cells, EPI-001 also acts as a PPAR-gamma modulator to result in inhibition of androgen receptor expression and activity, which inhibits prostate cancer growth. [2] |
| In vivo | In male mice bearing CRPC LNCaP s.c. xenografts, EPI-001 (50 mg/kg, i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth by reducing proliferation and increasing apoptosis. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 55 mg/mL (139.28 mM), Sonication is recommended.
Ethanol : 70 mg/mL (177.3 mM)
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| Keywords | Androgen | amino-terminal | anti-tumor | domain | EPI-001 | PPAR | inhibit | Peroxisome proliferator-activated receptors | PPARγ | Apoptosis | transactivation | Receptor | NTD | Androgen Receptor | Inhibitor |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Daidzein | Metronidazole | Sorafenib | Tributyrin | 2,3-Butanediol |
| Related Compound Libraries | Bioactive Compound Library | Anti-Diabetic Compound Library | Anti-Obesity Compound Library | Inhibitor Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Transcription Factor-Targeted Compound Library |
United States
