EPI-001

SKU: orb1300428

Description

EPI-001 is a small molecule that antagonizes the androgen receptor N-terminal domain (IC50 ~6 µM) and acts as a selective PPARγ modulator. It has been utilized in preclinical research to study prostate cancer mechanisms and metabolic pathways in both cellular and animal models.

Research Area

Cell Biology, Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 227947-06-0
• MW: 394.89
• Purity: 99.00% (May vary between batches)
• Formula: C₂₁H₂₇ClO₅
• SMILES: CC(C)(c1ccc(OCC(O)CO)cc1)c1ccc(OCC(O)CCl)cc1
• Target: Apoptosis|||Androgen Receptor|||PPAR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:55 mg/mL (139.28 mM);Ethanol:70 mg/mL (177.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.06 mM)

Bioactivity

• Target IC50:
  Androgen receptor:6 μM
• 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.
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• 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. 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

domain, Apoptosis, anti-tumor, AndrogenReceptor, Androgen Receptor, Androgen, amino-terminal, NTD, inhibit, Inhibitor, EPI001, EPI-001, EPI 001, Receptor, PPAR, Peroxisome proliferator-activated receptors, PPARγ, transactivation

Compound Identifiers

PubChem CID

4166922