EPI-001

Catalog No.S7955

For research use only.

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

EPI-001 Chemical Structure

CAS No. 227947-06-0

Selleck's EPI-001 has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.
Targets
PPARγ [2] Androgen Receptor [1]
(in LNCaP cells)
~6 μM
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]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: LNCaP cells
  • Concentrations: 10 μg/mL
  • Incubation Time: 4 days
  • Method: 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).
Animal Research:[1]
  • Animal Models: Male mice bearing LNCaP s.c. xenografts
  • Dosages: 50 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 394.89
Formula

C21H27ClO5

CAS No. 227947-06-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C1=CC=C(C=C1)OCC(CO)O)C2=CC=C(C=C2)OCC(CCl)O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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