Home Endocrinology & Hormones Androgen Receptor antagonist - PPAR modulator EPI-001 For research use only.

EPI-001

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

EPI-001 Chemical Structure

CAS No. 227947-06-0

Purity & Quality Control

EPI-001 Related Products

Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

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
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]
Cell Research 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).
In Vivo
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]
Animal Research Animal Models Male mice bearing LNCaP s.c. xenografts
Dosages 50 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 394.89 Formula

C21H27ClO5
CAS No. 227947-06-0 SDF Download EPI-001 SDF
Smiles CC(C)(C1=CC=C(C=C1)OCC(CO)O)C2=CC=C(C=C2)OCC(CCl)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (200.05 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble


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In vivo
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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.

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